Peptide Hormone Receptors

Products for:• Anterior Pituitary Regulation• Cardiovascular Regulation• Feeding and Appetite Regulation• Glucose Regulation• Other Peptide Hormones• Peptide Hormone Processing

Oriental Fire-bellied ToadBombina orientalisA source of Bombesin

Product Listing | Edition 2

Tocris Product Listing Series

2 |

ContentsThis listing contains over 200 products from Tocris that are used in the study of peptide hormone receptors, grouped by physiological activity; these include the regulation of the anterior pituitary gland, blood pressure, feeding, appetite and blood glucose levels. A product listing of nuclear receptor compounds is also available from www.tocris.com.

Anterior Pituitary Regulation . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . .4

Corticotropin-releasing Factor (CRF) Receptors .. . . . . . . . . . . 4

Gonadotropin-releasing Hormone (GnRH) Receptors .. . 4

Kisspeptin Receptors .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 5

Neurotensin (NT) Receptors .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 5

Somatostatin (sst) Receptors .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 5

Thyrotropin-releasing Hormone (TRH) Receptors .. . . . . . . . 5

Cardiovascular Regulation . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . .6

Angiotensin (AT) Receptors .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 6

Apelin (APJ) Receptors .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 6

Bradykinin Receptors .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 7

Calcitonin and Related Receptors .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 7

Endothelin (ET) Receptors .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 7

Natriuretic Peptide Receptors (NPR) ... . . . . . . . . . . . . . . . . . . . . . . . . . . . 8

Tachykinin (NK) Receptors .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 8

Urotensin-II (UT) Receptors .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 9

Vasopressin Receptors .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 10

Feeding and Appetite Regulation . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 10

Bombesin (BB) Receptors .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 10

CART ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 10

Cholecystokinin (CCK) Receptors .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 10

Galanin (GAL) Receptors .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 11

Ghrelin Receptors .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 11

GPR103 (QRFP Receptor) .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 11

GPR171 ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 12

GPR83 ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 12

Leptin Receptors .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 12

Melanin-concentrating Hormone (MCH) Receptors .. . . 12

Melanocortin (MC) Receptors .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 12

Motilin Receptors... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 13

Neuromedin U (NMU) Receptors .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 13

Neuropeptide B/W (NPBW) Receptors .. . . . . . . . . . . . . . . . . . . . . . . . 13

Neuropeptide S Receptors .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 13

Neuropeptide Y (NPY) Receptors .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 13

Orexin Receptors .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 14

Glucose Regulation . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 15

Amylin Receptors .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 15

Gastric Inhibitory Polypeptide (GIP) Receptors .. . . . . . . . . . 15

Glucagon Receptors .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 15

Glucagon-like Peptide 1 (GLP-1) Receptor .. . . . . . . . . . . . . . . . . 15

Glucagon-like Peptide 2 (GLP-2) Receptor .. . . . . . . . . . . . . . . . . 15

Insulin and Insulin-like Receptors .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 15

Other Peptide Receptors . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 16

Calcitonin Receptors .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 16

Mas-Related G Protein-Coupled Receptors .. . . . . . . . . . . . . . . . 16

Neuropeptide FF/AF Receptors .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 16

Opioid Receptors .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 17

Oxytocin Receptors .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 17

PACAP Receptors .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 18

Parathyroid Hormone Receptors .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 18

VIP Receptors .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 18

Peptide Hormone Processing . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 19

Aminopeptidases ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 19

Angiotensin-converting Enzymes (ACE) ... . . . . . . . . . . . . . . . . . . . . 19

Chymase ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 19

Dipeptidyl Peptidase IV (DPP IV) .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 19

Endothelin-converting Enzyme (ECE) ... . . . . . . . . . . . . . . . . . . . . . . . . 19

Insulin-degrading Enzyme (ICE) .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 19

Neurotensin-degrading Enzymes ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 19

Renin ... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 19

Tripeptidyl Peptidase II .. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 19

PEPTIDE HORMONE RECEPTORS

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IntroductionMost hormones are endogenous mediators secreted by endocrine glands as part of homeostasis. There are three types of hormone: peptide, steroid and amine hormones. Peptide hormones are generally hydrophilic molecules that do not freely diffuse across cell membranes; instead, most exert their effects by binding to cell-surface receptors in target tissues (Figure 1). Many peptide hormone receptors are coupled to heterotrimeric G proteins (that is, they are GPCRs). One notable exception is the insulin receptor, which possesses tyrosine kinase activity. Peptide receptors belong to the A and B classes of GPCRs, constituting a large group of receptors that are activated by extracellular protein or peptide ligands. Endogenous peptide receptor ligands bind to the N-terminus and/or the three extracellular loops of the receptor. The peptide receptor-binding domains are large, conferring high ligand affinity and specificity. Small molecule drugs, however, only bind to small discrete pockets or sites on these 7-transmembrane proteins.

Peptide hormones and their downstream effects are incredibly diverse; interactions within and between endocrine signaling pathways regulate a variety of interlinked processes, such as appetite modulation and feeding. Studying their activity therefore sheds light on a variety of different disorders. Research into endocrine disorders is facilitated by the use of agonists and antagonists active at peptide hormone receptors.

BrainAnterior Pituitary RegulationCRF ReceptorsGnRH ReceptorsKisspeptin ReceptorNeurotensin ReceptorsSomatostatin ReceptorsTRH Receptors

Heart, Arteries and KidneysCardiovascular RegulationAngiotensin ReceptorsApelin ReceptorsBradykinin ReceptorsCGRP ReceptorEndothelin ReceptorsNatriuretic Peptide ReceptorsTachykinin ReceptorsUrotensin-II ReceptorVasopressin Receptors

Liver and PancreasGlucose RegulationAmylin ReceptorGIP ReceptorGlucagon ReceptorGlucagon-like Peptide 1 ReceptorGlucagon-like Peptide 2 ReceptorInsulin and Insulin-like Receptors

Stomach and GutAppetite & Feeding RegulationBombesin ReceptorsCARTCCK ReceptorsGalanin ReceptorsGhrelin & Ghrelin-related ReceptorsGPR103 (QRFP Receptor)GPR171GPR83Leptin ReceptorsMCH ReceptorsMelanocortin ReceptorsMotilin Receptors Neuromedin U ReceptorsNeuropeptide B/W ReceptorsNeuropeptide S ReceptorNeuropeptide Y ReceptorsOrexin Receptors

Figure 1 | Peptide receptors involved in physiological processes

Tocris has a broad range of products for peptide hormone receptors, including small molecules and peptides. The information listed within is correct at the time of printing. For the latest information, and to request free scientific literature, please visit www.tocris.com.

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Anterior Pituitary RegulationThe anterior pituitary gland is regulated by hypothalamic hormones such as somatostatin, gonadotropin-releasing hormone and thyrotropin-releasing hormone. Stimulation by the hypothalamus influences the release of hormones from the anterior pituitary, including growth hormone, prolactin and adrenocorticotropic hormone (ACTH).

High Affinity CRF1 Receptor Antagonist

R 121919 Cat. No. 6530

R 121919 is a high affinity corticotropin release factor receptor 1 (CRF1) antagonist (Ki = 3.5 nM). It reduces stress-induced elevations of plasma ACTH in rats. R 121919 also dispays anxiolytic and antidepressant effects in vivo, and it is orally bioavailable

N

N

NN

N

N

R 121919 Cat. No. 6530

Potent and Selctive CRF1 Antagonist

CP 376395 Cat. No. 3212

CP 376395 is an orally active, potent and selective corticotropin release factor receptor 1 (CRF1) antagonist (Ki values are 12 and >10000 nM for CRF1 and CRF2, respectively). It attenuates CRF-induced activation of the HPA axis in vivo.

N O

NH

CP 376395 Cat. No. 3212

Corticotropin-releasing Factor Receptors

Agonists 6450 Cortagine Potent and selective CRF1 agonist 100 µg

1151 CRF (human, rat) Stimulates ACTH release 200 µg

1609 Sauvagine CRF agonist 500 µg

1608 Stressin I CRF1 agonist 500 µg

1604 Urocortin (human) Endogenous CRF agonist 1 mg

1605 Urocortin (rat) Endogenous CRF agonist 1 mg

Antagonists 2778 Antalarmin CRF1 antagonist 10 mg

50 mg

2071 Antisauvagine-30 Potent, selective and competitive CRF2 antagonist 1 mg

1606 Astressin Potent CRF antagonist 500 µg

2391 Astressin 2B Selective CRF2 antagonist 500 µg

2779 CP 154526 Selective, non-peptide CRF1 antagonist 10 mg

50 mg

3212 CP 376395 Potent and selective CRF1 antagonist 10 mg

50 mg

1184 α-helical CRF 9-41 CRF antagonist 500 µg

2070 K 41498 Highly selective and potent CRF2 antagonist 1 mg

1591 NBI 27914 Selective non-peptide CRF1 antagonist 10 mg

50 mg

3100 NBI 35965 Potent and selective CRF1 antagonist 10 mg

50 mg

6451 Pexacerfont Potent and selective CRF1 antagonist; anxiolytic 10 mg

50 mg

6530 R 121919 High affinity CRF1 antagonist; orally bioavailable 10 mg

50 mg

3294 SN 003 Potent and selective CRF1 antagonist 10 mg

Other 1607 CRF (6-33) CRF-binding protein inhibitor 1 mg

Gonadotrophin-releasing Hormone Receptors

Agonists 3592 Goserelin acetate GnRH receptor agonist 10 mg

2873 Leuprolide GnRH receptor agonist 1 mg

2544 Nafarelin GnRH receptor agonist 1 mg

Category Cat. No. Product Name Description Unit Size

PEPTIDE HORMONE RECEPTORS

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Antagonists 2730 AG 045572 Selective GnRH receptor antagonist 1 mg

10 mg

3536 Cetrorelix Acetate Potent GnRH receptor antagonist 1 mg

2519 T 98475 GnRH receptor antagonist 1 mg

Kisspeptin Receptors

Agonists 2570 Kisspeptin 10 (human) Endogenous ligand for kisspeptin receptor 1 mg

4243 Kisspeptin 10 (rat) Endogenous ligand for kisspeptin receptor 1 mg

1443 Metastin (human) Potent, endogenous ligand for kisspeptin receptor 100 µg

Antagonists 3881 Kisspeptin 234 Kisspeptin receptor antagonist; kisspeptin 10 (Cat. No. 2570) analog 1 mg

Neurotensin Receptors

Agonists 1998 JMV 449 Potent neurotensin receptor agonist 1 mg

1909 Neurotensin Endogenous neurotransmitter and endocrine modulator 1 mg

5087 TC NTR1 17 Selective NTS1 partial agonist 10 mg

50 mg

Antagonists 5438 NTRC 824 Potent and selective non-peptide NTS2 antagonist 10 mg

50 mg

2309 SR 142948 Highly potent NTS receptor antagonist 1 mg

10 mg

3721 SR 48692 Selective non-peptide NTS1 antagonist 5 mg

25 mg

Somatostatin Receptors

Agonists 2454 CH 275 Potent and selective sst1 agonist 500 µg

2444 (1R,1’S,3’R/1R,1’R,3’S)-L-054,264 Potent and selective sst2 agonist 1 mg

10 mg

1979 L-803,087 Potent and selective sst4 agonist 10 mg

1980 L-817,818 Potent and selective sst5 agonist 10 mg

2440 NNC 26-9100 Selective sst4 agonist 10 mg

1818 Octreotide sst2, sst3 and sst5 agonist 1 mg

1157 Somatostatin Influences growth hormone release 1 mg

1165 Somatostatin 1-28 sst agonist 500 µg

5080 TC-G 1003 High affinity somatostatin sst2 receptor agonist 10 mg

4639 TT 232 sst1 and sst4 agonist 1 mg

Antagonists 3493 Cyclosomatostatin Non-selective sst antagonist 1 mg

1843 CYN 154806 Selective sst2 antagonist 1 mg

Other 1844 BIM 23056 sst ligand 1 mg

3374 Cortistatin 14 Endogenous neuropeptide; binds sst1 – sst5 and ghrelin receptor 1 mg

Thyrotropin-releasing Hormone Receptors

Agonists 2672 Taltirelin Synthetic thyrotropin-releasing hormone analog 1 mg

10 mg

D-Phe-His-Leu-Leu-Arg-Lys-Met-Ile-Glu-Ile-Glu-Lys-Gln-Glu-Lys-Glu-Lys-Gln-Gln-Ala-

Ala-Asn-Asn-Arg-Leu-Leu-Leu-Asp-Thr-Ile-NH2

Antisauvagine-30 (2071)Potent, selective and competitive CRF2 antagonist

N

HNO

O

NH

O

N

OO

NH2

N

HN

Taltirelin (2672)Synthetic TRH analog

NH

HN NH2

NH

OO OMeHNF

F

L-803,087 (1979)Potent and selective sst4 agonist

Key Products for Anterior Pituitary Regulation

Category Cat. No. Product Name Description Unit Size

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Angiotensin Receptors

Agonists 1562 Angiotensin (1-7) Vasorelaxant peptide 1 mg

1563 Angiotensin I (human, mouse, rat) Endogenous precursor to angiotensin II (Cat. No. 1158) 1 mg

1158 Angiotensin II Potent vasoconstrictor peptide 5 mg

Inverse Agonists

4553 Azilsartan Potent AT1 receptor inverse agonist; antihypertensive 10 mg

50 mg

Antagonists 4791 Candesartan AT1 receptor antagonist 10 mg

50 mg

1849 EMD 66684 Potent, selective non-peptide AT1 antagonist 10 mg

50 mg

5728 EXP 3174 Potent and selective AT1 receptor antagonist 10 mg

50 mg

3798 Losartan potassium Selective, non-peptide AT1 antagonist 50 mg

4616 Olmesartan Potent AT1 antagonist 50 mg

1361 PD 123319 Potent and selective non-peptide AT2 antagonist 10 mg

50 mg

4216 Valsartan High affinity, selective AT1 antagonist 10 mg

50 mg

1211 ZD 7155 Selective non-peptide AT1 antagonist 10 mg

50 mg

Ligands 2569 CGP 42112 Selective, high affinity AT2 ligand 1 mg

Apelin Receptors

Agonists 2420 [Pyr1]-Apelin-13 Potent peptide agonist for APJ receptor 1 mg

3007 Apelin-17 (human, bovine) Endogenous APJ receptor agonist 1 mg

2426 Apelin-36 (human) Endogenous APJ receptor agonist 1 mg

2427 Apelin-36 (rat, mouse) Endogenous APJ receptor agonist 1 mg

6698 ELA-11 (human) High affinity apelin receptor agonist 1 mg

6293 ELA-14 (human) Potent apelin (APJ) receptor agonist 1 mg

6697 ELA-21 (human) High affinity apelin receptor agonist 1 mg

6291 ELA-32 (human) Potent, high affinity apelin receptor agonist; stimulates angiogenesis 100 µg

5966 ML 233 Non-peptide apelin receptor agonist 10 mg

50 mg

Cardiovascular RegulationBlood pressure may vary in response to factors such as diet, exercise and stress. Key hormones that regulate this response include angiotensin, endothelin and vasopressin. Feedback of the renin-angiotensin system to the posterior pituitary prompts the release of vasopressin, increasing blood pressure.

Glp-Arg-Pro-Arg-Leu-Ser-His-Lys-Gly-Pro-Met-Pro-Phe

O

O

S

O

OO2N

N

N

Gln-Arg-Pro-Val-Asn-Leu-Thr-Met-Arg-Arg-Lys-Leu-Arg-Lys-His-Asn-Cys-Leu-Gln-Arg-

Arg-Cys-Met-Pro-Leu-His-Ser-Arg-Val-Pro-Phe-Pro

Glp-Arg-Arg-Cys-Met-Pro-Leu-His-Ser-Arg-Val-Pro-Phe-Pro

{Pyr1}-Apelin-13 (2420)Potent peptide apelin agonist

ELA-32 (Human) (6291)Potent and high affinity apelin agonist

stimulates angiogenesis

ELA-14 (Human) (6293)Potent apelin agonist

ML 221 (4748)Apelin antagonist

Key Products for Apelin Receptors

Category Cat. No. Product Name Description Unit Size

PEPTIDE HORMONE RECEPTORS

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Antagonists 4748 ML 221 Apelin receptor (APJ) antagonist 10 mg

50 mg

5992 MM 54 Potent apelin receptor antagonist 1 mg

Controls 6294 ELA-14 negative control Negative control for ELA-14 (Cat. No. 6293) 1 mg

6292 ELARR>GG Negative control for ELA-32 (Cat. No. 6291) 100 µg

Bradykinin Receptors

Agonists 3004 Bradykinin Endogenous agonist at bradykinin receptors (B2 > B1) 5 mg

3005 [Des-Arg9]-Bradykinin Bradykinin receptor agonist (B1 > B2) 5 mg

3229 [Phe8Ψ(CH-NH)-Arg9]-Bradykinin Selective B2 agonist 1 mg

3230 Sar-[D-Phe8]-des-Arg9-Bradykinin Potent and selective B1 agonist 1 mg

Antagonists 3014 HOE 140 Potent and selective B2 antagonist 500 µg

3978 MEN 11270 Selective B2 antagonist; analog of HOE 140 (Cat. No. 3014) 500 µg

3407 R 715 Potent and selective B1 antagonist 1 mg

3226 R 892 Potent and selective B1 antagonist 1 mg

1057 WIN 64338 Bradykinin B2 antagonist 10 mg

50 mg

Other 2370 Bombinakinin-GAP Bioactive, bradykinin-related peptide 1 mg

6190 Retrobradykinin Reverse analog of Bradykinin 1 mg

Calcitonin and Related Receptors

Agonists 3012 α-CGRP (human) CGRP receptor agonist 1 mg

1161 CGRP (rat) Potent vasodilator 100 µg

Antagonists 4561 BIBN 4096 Potent and selective CGRP receptor antagonist 10 mg

1181 CGRP 8-37 (human) CGRP receptor antagonist 500 µg

1169 CGRP 8-37 (rat) CGRP receptor antagonist 500 µg

4314 SB 268262 Selective non-peptide CGRP antagonist 10 mg

50 mg

Endothelin Receptors

Agonists 1189 BQ-3020 Selective ETB agonist 500 µg

1160 Endothelin 1 (human, porcine) Endothelin receptor agonist; potent vasoconstrictor peptide 100 µg

1164 Endothelin 2 (human) Endothelin receptor agonist 100 µg

1162 Endothelin 3 (human, rat) Endothelin receptor agonist; potent vasoconstrictor 100 µg

1196 IRL-1620 Highly selective ETB agonist 500 µg

1175 Sarafotoxin S6c Selective ETB agonist 100 µg

N

N

N

NMe2

Me

Ph2HC

O

HO2C

PD 123319 (1361)Potent and selective non-peptide AT2 antagonist

N

NN

KN

NN

Cl

HO

Cys-Ser-Cys-Ser-Ser-Leu-Met-Asp-Lys-Glu-

Cys-Val-Tyr-Phe-Cys-His-Leu-Asp-lle-Ile-Trp

N

NO

OHO

MeO

Losartan potassium (3798)Selective non-peptide AT1 antagonist

Endothelin 1 (human, porcine) (1160)Endothelin receptor agonist; potent vasocontrictor peptide

Ambrisentan (5828)Selective ETA antagonist

NH

HN

O

N

OO NH

Me3C

Me

Me

N

OMeO

NaO2C

BQ 788 (1500)Selective ETB antagonist

Key Products for Angiotensin and Endothelin Receptors

Category Cat. No. Product Name Description Unit Size

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Antagonists 5730 A 127722 Highly potent, selective ETA antagonist; orally bioavailable 10 mg

5828 Ambrisentan Selective ETA antagonist 10 mg

50 mg

1441 BMS 182874 Highly selective ETA antagonist; orally active 10 mg

50 mg

6232 Bosentan High affinity endothelin receptor antagonist; orally bioavailable 10 mg

50 mg

1500 BQ 788 sodium salt Selective ETB antagonist 1 mg

1188 BQ-123 Selective ETA antagonist 500 µg

1210 FR 139317 Highly potent and selective ETA antagonist 10 mg

50 mg

1838 IRL-2500 Potent ETB antagonist 10 mg

Natriuretic Peptide Receptors

Agonists 6715 A 71915 Highly potent and competitive NPRA antagonist 1 mg

1906 Atrial natriuretic factor (1-28) (human, porcine)

Endogenous peptide regulating blood pressure 1 mg

1912 Atrial natriuretic factor (1-28) (rat) Endogenous peptide regulating blood pressure 1 mg

3522 Brain natriuretic peptide (1-32) (human)

Endogenous peptide agonist at ANP receptor A (NPR1) 1 mg

3520 C-type natriuretic peptide (1-22) (human, rat, swine)

Endogenous peptide agonist at NPR2 500 µg

Antagonists 5498 AP 811 High affinity and selective NPR3 antagonist 1 mg

Tachykinin (NK) Receptors

Agonists 1668 GR 64349 Potent and selective NK2 agonist 1 mg

1669 GR 73632 Potent and selective NK1 agonist 1 mg

2576 Hemokinin 1 (human) Endogenous selective NK1 agonist 1 mg

1535 Hemokinin 1 (mouse) Endogenous high affinity and selective NK1 agonist 1 mg

1640 [bAla8]-Neurokinin A(4-10) NK2 agonist 1 mg

3228 [Lys5,MeLeu9,Nle10]-NKA(4-10) Selective NK2 agonist 1 mg

1582 Neurokinin B (human, porcine) Endogenous tachykinin peptide 1 mg

1068 Senktide NK3 agonist 500 µg

1156 Substance P Sensory neuropeptide; inflammatory mediator 5 mg

1178 [Sar9,Met(O2)11]-Substance P Potent and selective NK1 agonist 1 mg

Antagonists 1954 Antagonist G Broad spectrum neuropeptide receptor antagonist 1 mg

6486 Aprepitant Potent long-acting hNK1 antagonist 50 mg

3649 CP 122721 High affinity NK1 receptor antagonist 5 mg

25 mg

NHN

N

HNO

O

HNN N N

O O

NH2

Br

Br

HO

BIBN 4096 (4561)Potent and selective CGRP antagonist

Ac-Lys-Arg-Pro-Pro-Gly-Phe-Ser-DβNal-Ile

R 715 (3407)Potent and selective B1 antagonist

Gly-Leu-Ser-Lys-Gly-Cys-Phe-Gly-Leu-Lys-Leu-Asp-Arg-Ile-Gly-Ser-Met-Ser-Gly-Leu-

Gly-Cys

Arg-Cys-Cha-Gly-Gly-Arg-Ile-Asp-Arg-Ile-

D-Tic-Arg-Cys-NH2

O

O

S OO

NO

N

OH

ON

ClO

A 71915 (6715)Highly potent and competitive NPRA antagonist

C-type natriuretic peptide (1-22) (human, rat, swine) (3520)Endogenous peptide agonist at NPR2

SSR 149415 (6195)Potent and selective vasopressin

V1B antagonist

Key Products for Other Cardiovascular Peptide Receptors

Category Cat. No. Product Name Description Unit Size

PEPTIDE HORMONE RECEPTORS

www.tocris.com | 9

2893 CP 96345 Potent and selective NK1 antagonist 10 mg

50 mg

3417 CP 99994 High affinity NK1 antagonist 10 mg

50 mg

2400 FK 888 High affinity NK1 antagonist 10 mg

1274 GR 159897 Potent NK2 antagonist 10 mg

50 mg

4647 GR 203040 Potent and selective NK1 antagonist 5 mg

25 mg

1667 GR 94800 Potent and selective NK2 antagonist 1 mg

4013 L 760735 High affinity NK1 antagonist 10 mg

50 mg

0868 L-732,138 Potent and selective NK1 antagonist 10 mg

50 mg

1145 L-733,060 Potent NK1 antagonist 10 mg

50 mg

1632 MEN 10376 Potent and selective NK2 antagonist 1 mg

1635 RP 67580 Potent and selective NK1 antagonist 10 mg

50 mg

1376 SB 218795 Potent and selective NK3 antagonist 10 mg

50 mg

1393 SB 222200 Potent and selective NK3 antagonist; brain penetrant 10 mg

50 mg

1784 Spantide I Selective NK1 antagonist 1 mg

4012 SR 140333 Potent NK1 antagonist 10 mg

50 mg

1946 [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P

Substance P analog and broad spectrum neuropeptide receptor antagonist/inverse agonist; anticancer in vitro

1 mg

Urotensin-II Receptors

Agonists 1642 Urotensin II (human) Endogenous urotensin II (UT) agonist; vasoactive 1 mg

Antagonists 5110 GSK 1562590 High affinity, selective urotensin II (UT) antagonist 10 mg

50 mg

4670 SB 611812 Urotensin-II (UT) antagonist; attenuates cardiac dysfunction 10 mg

50 mg

3571 SB 657510 Selective urotensin-II (UT) antagonist 10 mg

50 mg

4667 SB 706375 High affinity, non-peptide urotensin-II (UT) antagonist 10 mg

50 mg

Vasopressin Receptors

Agonists 3396 Desmopressin V1B and V2 agonist; synthetic vasopressin analog 1 mg

2935 [Arg8]-Vasopressin Endogenous vasopressin agonist; antidiuretic hormone 1 mg

3127 d[Leu4,Lys8]-VP Selective V1B agonist 1 mg

Antagonists 6830 Conivaptan Very high affinity vasopressin V1A and V2 antagonist; orally bioavailable 10 mg

50 mg

3924 OPC 21268 V1 antagonist; orally active 10 mg

50 mg

2310 SR 49059 Selective V1A antagonist; orally active 10 mg

6195 SSR 149415 Potent and selective V1B antagonist 10 mg

50 mg

5729 TASP 0390325 Potent and selective V1B antagonist; orally bioavailable 10 mg

50 mg

5181 Tolvaptan Potent and selective V2 antagonist; renoprotective and orally active 10 mg

50 mg

3377 (d(CH2)51,Tyr(Me)2,Arg8)-

VasopressinSelective V1A antagonist 1 mg

Other 4625 TC OT 39 V1A antagonist; also oxytocin and V2 receptor partial agonist 10 mg

Cardiovascular Regulation – continued

Category Cat. No. Product Name Description Unit Size

Tocris Product Listing Series

10 |

Bombesin Receptors

Agonists 5600 BA 1 Potent bombesin agonist 1 mg

2716 BIM 187 Bombesin agonist 1 mg

1149 Bombesin Bombesin agonist; involved in gastrointestinal tract function 1 mg

1789 GRP (human) Endogenous BB2 agonist 1 mg

1788 GRP (porcine) Endogenous BB2 agonist 1 mg

1908 Neuromedin B (porcine) Endogenous mammalian BB1 agonist 1 mg

Antagonists 2717 BIM 189 Bombesin antagonist 1 mg

3237 BIM 23042 Selective BB1 antagonist 1 mg

5599 ML 18 BB3 antagonist; also binds BB2 10 mg

2602 PD 176252 Highly potent BB1 and BB2 antagonist 10 mg

CART

Other 3338 CART (55-102) (human) Neuromodulatory neuropeptide fragment; satiety factor 100 µg

3337 CART (55-102) (rat) Neuromodulatory neuropeptide fragment; satiety factor 100 µg

3339 CART (62-76) (rat, human) Neuromodulating neuropeptide fragment; inhibits food intake in vivo 1 mg

Cholecystokinin (CCK) Receptors

Agonists 2411 A-71623 Potent and selective CCK1 agonist; suppresses feeding 1 mg

6264 Caerulein CCK agonist 1 mg

1150 CCK Octapeptide, non-sulfated Non-sulfated form of CCK octapeptide 1 mg

1166 CCK Octapeptide, sulfated C-terminal octapeptide of CCK 1 mg

3006 Gastrin I (human) Selective CCK2 agonist 1 mg

Antagonists 2607 CI 988 Potent and selective CCK2 antagonist 10 mg

50 mg

2304 Devazepide Selective CCK1 antagonist; orally active 10 mg

50 mg

2767 L-365,260 Selective CCK2 antagonist 10 mg

50 mg

3036 Loxiglumide CCK1 antagonist; active in vivo 5 mg

25 mg

1524 LY 288513 Selective CCK2 antagonist 10 mg

50 mg

1478 Proglumide sodium salt Non-selective CCK antagonist; orally active 50 mg

2190 SR 27897 Potent and selective CCK1 antagonist 10 mg

50 mg

1408 YM 022 Highly potent and selective CCK2 antagonist 10 mg

50 mg

Feeding and Appetite RegulationFeeding and appetite modulation are key targets in antiobesity research. In particular, leptin, ghrelin and orexin sense and regulate energy levels in the body. Other appetite-regulating peptides include opioids, which stimulate feeding. Gastrointestinal hormones such as cholecystokinin influence digestion following food intake.

N

NO

HN

NH

O

Devazepide (2304)Selective, orally active CCK1 antagonist

Gly-Trp-Thr-Leu-Asn-Ser-Ala-Gly-Tyr-Leu-Leu-Gly-Pro-His-Ala-Ile-Asp-Asn-His-Arg-

Ser-Phe-Ser-Asp-Lys-His-Gly-Leu-Thr-NH2

Galanin (1-29) (rat, mouse) (2696)Non-selective galanin receptor agonist

Gly-Ser-Ser-Phe-Leu-Ser-Pro-Glu-His-Gln-Lys-Ala-Gln-Gln-Arg-Lys-Glu-Ser-Lys-Lys-

Pro-Pro-Ala-Lys-Leu-Gln-Pro-Arg

nOctanoyl

Ghrelin (rat) (1465)Endogenous ghrelin receptor agonist

Glp-Gln-Asp-Tyr(SO H)-Thr-Gly-Trp-Met-3Asp-Phe-NH2

Caerulein (6264)CCK agonist

N

N

O

O

N

F

YIL 781 (3959)Ghrelin receptor (GHS-R1a) antagonist

Key Products for CCK, Galanin and Ghrelin Receptors

Category Cat. No. Product Name Description Unit Size

PEPTIDE HORMONE RECEPTORS

www.tocris.com | 11

Galanin Receptors

Agonists 2699 AR-M 1896 GAL2 agonist 1 mg

1450 Galanin (1-15) (porcine, rat) Galanin receptor agonist peptide 1 mg

2696 Galanin (1-29) (rat, mouse) Non-selective galanin agonist 1 mg

1179 Galanin (1-30) (human) Endogenous galanin agonist 200 µg

1451 Galanin (2-29) (rat) Selective GAL2 peptide agonist 1 mg

3008 Galanin (porcine) Endogenous galanin agonist 1 mg

2085 Galnon Non-selective galanin agonist 10 mg

3629 M 1145 Potent and selective GAL2 agonist 500 µg

2697 M617 Selective GAL1 agonist 1 mg

6090 Spexin Potent GAL2 and GAL3 agonist; exhibits anxiolytic effects in vivo 1 mg

Antagonists 3425 M40 Potent non-selective galanin antagonist 1 mg

2698 M871 Selective GAL2 antagonist 1 mg

5426 SNAP 398299 Potent and selective GAL3 antagonist 5 mg

Ghrelin Receptors

Agonists 1463 Ghrelin (human) Endogenous ghrelin agonist 1 mg

1465 Ghrelin (rat) Endogenous ghrelin agonist 1 mg

2261 L-692,585 Potent, non-peptide ghrelin agonist 10 mg

2308 Tabimorelin Potent ghrelin agonist; orally active 10 mg

Inverse Agonists

5830 K-(d-1-Nal)-FwLL-NH2 High affinity and potent ghrelin inverse agonist 1 mg

6347 PF 04628935 Potent ghrelin inverse agonist 5 mg

25 mg

6350 PF 05190457 High affinity and selective ghrelin inverse agonist 5 mg

25 mg

Antagonists 1922 [D-Lys3]-GHRP-6 Ghrelin antagonist 5 mg

3959 YIL 781 Ghrelin antagonist 5 mg

25 mg

Other 3374 Cortistatin 14 Endogenous neuropeptide; binds sst1 – sst5 and ghrelin receptor 1 mg

2260 [Des-octanoyl]-Ghrelin (human) Major circulating form of ghrelin; devoid of activity at ghrelin receptor but is active in vivo

1 mg

2951 [Des-octanoyl]-Ghrelin (rat) Major circulating form of ghrelin; devoid of activity at GHS receptor 1 mg

5560 Obestatin (human) Endogenous reported anorexigenic peptide 1 mg

GPR103

Ligands 4402 26RFa Ligand of GPR103; orexigenic neuropeptide 1 mg

Potent Galanin Receptor Agonist

Spexin Cat. No. 6090

Spexin is a potent galanin receptor 2 and 3 (GAL2/GAL3) agonist (EC50 values are 45.7 and 112.2 nM, respectively. This compound exhibits no significant activity at GAL1 receptors. In mice and rats with diet-induced obesity, spexin inhibits long chain fatty acid uptake by adipoctyes and decreases food intake. It also exhibits anxiolytic effects in vivo.

Asn-Trp-Thr-Pro-Gln-Ala-Met-Leu-Tyr-Leu-Lys-Gly-Ala-Gln-NH2

Spexin Cat. No. 6090

Selective non-peptide OX1 Antagonist

SB 334867 Cat. No. 1960

SB 334867 is a selective non-peptide orexin OX1 receptor antagonist (pKb = 7.2 for inhibition of intracellular Ca2+ release in CHO cells expressing human OX1). This compound blocks orexin A-induced grooming and feeding following systemic administration in vivo.

HN

O N

OMe

N

N

HN

SB 334867 Cat. No. 1960

Category Cat. No. Product Name Description Unit Size

Tocris Product Listing Series

12 |

GPR171

Agonists 6304 BigLEN (mouse) GPR171 agonist 1 mg

6306 BigLEN (rat) Potent GPR171 agonist 1 mg

6299 MS 15203 Potent and selective GPR171 partial agonist 5 mg

25 mg

Antagonists 6298 MS 21570 GPR171 antagonist 10 mg

50 mg

GPR83

Agonists 6307 PEN (human) GPR83 agonist 1 mg

6308 PEN (mouse) GPR83 agonist 1 mg

6309 PEN (rat) GPR83 agonist 1 mg

Leptin Receptors

Others 2985 LEP (116-130) (mouse) Synthetic leptin peptide fragment 1 mg

Melanin-concentrating Hormone Receptors

Agonists 3434 [Ala17]-MCH Potent MCH receptor agonist 1 mg

3806 MCH (human, mouse, rat) Potent endogenous MCH agonist 100 µg

Antagonists 3346 ATC 0175 MCH1 antagonist; also 5-HT2B antagonist and 5-HT1A partial agonist 10 mg

50 mg

4242 GW 803430 MCH1 antagonist 10 mg

50 mg

3347 SNAP 94847 Potent and selective MCH1 antagonist 10 mg

50 mg

4365 TC-MCH 7c Selective MCH1 antagonist 10 mg

Melanocortin Receptors

Agonists 3492 ACTH (1-39) Potent endogenous MC2 agonist 1 mg

4053 BMS 470539 Potent, selective MC1 receptor agonist 10 mg

50 mg

2566 Melanotan II High affinity melanocortin agonist 1 mg

3013 [Nle4,D-Phe7]-α-MSH Melanocortin agonist; synthetic analog of α-MSH (Cat. No. 3013) 1 mg

4272 [D-Trp8]-γ-MSH Selective MC3 agonist 1 mg

5094 PG 931 Potent and selective MC4 agonist 1 mg

3032 THIQ Potent and selective MC4 agonist 1 mg

2584 α-MSH Endogenous melanocortin agonist 1 mg

3424 γ1-MSH Selective MC3 agonist 1 mg

pGlu-Pro-Leu-Pro-Asp-Cys-Cys-Arg-Gln-Lys-

Thr-Cys-Ser-Cys-Arg-Leu-Tyr-Glu-Leu-Leu-His-Gly-Ala-Gly-Asn-His-Ala-Ala-Gly-Ile-

Leu-Thr-Leu-NH2

Orexin A (human, rat, mouse) (1455)Endogenous agonist at OX1 and OX2

Ser-Tyr-Ser-Met-Glu-His-Phe-Arg-Trp-Gly-Lys-Pro-Val-Gly-Lys-Lys-Arg-Arg-Pro-Val-Lys-Val-Tyr-Pro-Asn-Gly-Ala-Glu-Asp-Glu-Ser-Ala-Glu-Ala-Phe-Pro-Leu-Glu-Phe

ACTH (1-39) (3492)Potent endogenous MC2 agonist

N

NN

N

O

HN O

HN

ClTHIQ (3032)

Potent and selective MC4 receptor agonist

NMeO

MeO

OMe

MeO

O

HN

ACT 335827 (4983)Potent and selective OX1 antagonist

Key Products for Melanocortin and Orexin Receptors

Category Cat. No. Product Name Description Unit Size

PEPTIDE HORMONE RECEPTORS

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Feeding and Appetite Regulation – continued

Tyr-Pro-Ser-Lys-Pro-Asp-Asn-Pro-Gly-Glu-Asp-Ala-Pro-Ala-Glu-Asp-Met-Ala-Arg-Tyr-Tyr-Ser-Ala-Leu-Arg-His-Tyr-Ile-Asn-Leu-

Leu-Thr-Arg-Pro-Arg-Tyr-NH2

[Leu31,Pro34]-Neuropeptide Y (human, rat) (1176)

NPY Y1 receptor agonist

NH N

H

O

HN O

HN NH2

O

NH2

NH

BIBO 3304 (2412)Highly selective NPY Y1

receptor antagonist

N NH

N

HN

O

O O

O

HN

NNN

O

O

HN

H2N NH

BIIE 0246 (1700)Potent, selective non-peptide NPY Y2 receptor antagonist

Key Products for Neuropeptide Y Receptors

Antagonists 1831 HS 014 Selective MC4 antagonist 1 mg

1832 HS 024 Highly potent MC4 antagonist 1 mg

3438 MCL 0020 Selective MC4 antagonist 1 mg

4854 ML 00253764 MC4 antagonist; brain penetrant 10 mg

50 mg

Modulators 6926 Fenoprofen Positive allosteric modulator of MC3 receptors; exhibits biased signaling 50 mg

Other 5954 MSG 606 Potent human MC1 antagonist; also MC3 and MC5 partial agonist 1 mg

3420 SHU 9119 MC3 and MC4 antagonist; MC5 partial agonist 1 mg

Motilin Receptors

Agonists 2264 Motilin (human, porcine) Endogenous peptide regulator of gastrointestinal motility 1 mg

Antagonists 5074 ANQ 11125 Selective motilin receptor antagonist 1 mg

4934 MA 2029 Potent and selective, competitive motilin antagonist; orally active 10 mg

50 mg

Neuromedin U Receptors

Agonists 3648 Neuromedin S (rat) Potent endogenous NMU1 and NMU2 agonist 500 µg

1917 Neuromedin U (rat) Endogenous modulator of blood pressure and flow, gut ion transport, feeding and body temperature

1 mg

Neuropeptide B/W Receptors

Agonists 3009 Neuropeptide W-23 (human) Endogenous NPBW1 and NPBW2 receptor agonist 1 mg

Neuropeptide S Receptors

Agonists 5857 Neuropeptide S (Mouse) Endogenous neuropeptide S agonist 1 mg

Antagonists 5161 ML 154 Potent neuropeptide S antagonist 10 mg

50 mg

4510 SHA 68 Selective neuropeptide S antagonist 10 mg

50 mg

Neuropeptide Y Receptors

Agonists 1153 Neuropeptide Y (human, rat) Endogenous NPY agonist; influences feeding and sexual behavior 200 µg

1176 [Leu31,Pro34]-Neuropeptide Y (human, rat)

NPY Y1 agonist 200 µg

1173 Neuropeptide Y (porcine) Endogenous NPY agonist; influences feeding and sexual behavior 200 µg

1177 Neuropeptide Y 13-36 (porcine) NPY Y1 agonist 500 µg

1154 Pancreatic Polypeptide (human) NPY Y4 agonist; involved in gastrointestinal tract function 200 µg

1365 [cPP1-7,NPY19-23,Ala31,Aib32, Gln34] - hPancreatic Polypeptide

Potent and selective NPY Y5 agonist 1 mg

1618 Peptide YY (3-36) Selective NPY Y2 agonist 500 µg

6288 Peptide YY (3-36) human NPY Y2 agonist 500 µg

Category Cat. No. Product Name Description Unit Size

Tocris Product Listing Series

14 |

Feeding and Appetite Regulation – continued

Antagonists 2412 BIBO 3304 Highly selective NPY Y1 antagonist 10 mg

50 mg

2707 BIBP 3226 trifluoroacetate Mixed NPY Y1 and NPFF antagonist 1 mg

10 mg

1700 BIIE 0246 Potent and selective non-peptide NPY Y2 antagonist 1 mg

10 mg

3242 BMS 193885 Potent competitive NPY Y1 antagonist 10 mg

50 mg

2199 CGP 71683 Highly selective and potent non-peptide NPY Y5 antagonist 10 mg

50 mg

4606 CYM 9484 Potent NPY Y2 antagonist 10 mg

50 mg

4018 JNJ 5207787 Selective NPY Y2 antagonist 10 mg

50 mg

3562 LU AA33810 Potent NPY Y5 antagonist 10 mg

50 mg

3677 NPY 5RA972 Potent and selective NPY Y5 antagonist 10 mg

50 mg

2200 PD 160170 Selective non-peptide NPY Y1 antagonist 10 mg

3898 SF 11 NPY Y2 antagonist 10 mg

50 mg

Modulators 6411 tBPC Positive allosteric modulator of NPY Y4 receptor 10 mg

50 mg

Controls 3903 Neuropeptide Y (scrambled) Control peptide for neuropeptide Y (Cat. No. 1173) 1 mg

Others 1486 GR 231118 Potent NPY Y1 antagonist and Y4 agonist; also binds to NPFF receptors 500 µg

Orexin Receptors

Agonists 2142 [Ala11,D-Leu15]-Orexin B Potent and selective OX2 agonist 1 mg

1455 Orexin A (human, rat, mouse) Endogenous agonist at orexin receptors 500 µg

1456 Orexin B (human) Endogenous agonist at orexin receptors 500 µg

1457 Orexin B (mouse) Endogenous agonist at orexin receptors 500 µg

5115 OXA (17-33) Potent and selective peptide OX1 agonist 1 mg

Antagonists 4983 ACT 335827 Potent and selective OX1 antagonist 10 mg

50 mg

4558 EMPA Highly potent and selective OX2 antagonist; brain penetrant 10 mg

50 mg

4317 JNJ 10397049 Selective OX2 antagonist 10 mg

50 mg

1960 SB 334867 Selective non-peptide OX1 antagonist 1 mg

10 mg

50 mg

1963 SB 408124 Selective non-peptide OX1 antagonist 10 mg

3818 TCS 1102 Potent orexin receptor antagonist 10 mg

50 mg

3371 TCS OX2 29 Potent and selective OX2 antagonist 10 mg

50 mg

Category Cat. No. Product Name Description Unit Size

PEPTIDE HORMONE RECEPTORS

www.tocris.com | 15

Amylin Receptors

Agonists 3418 Amylin Endogenous peptide agonist for amylin, calcitonin, CGRP and adrenomedullin receptors

500 µg

6030 Amylin (rat) Potent endogenous peptide agonist for amylin, calcitonin, CGRP and adrenomedullin receptors

500 µg

5031 Pramlintide Amylin agonist; synthetic version of amylin (Cat. No. 3418) 500 µg

Antagonists 3419 AC 187 Potent and selective amylin antagonist 500 µg

6550 AC 253 Amylin antagonist 1 mg

6549 cAC 253 Amylin (AMY3) antagonist; brain penetrant 500 µg

Gastric Inhibitory Polypeptide Receptors

Agonists 6699 {D-Ala2}-GIP (human) Highly potent GIP agonist 1 mg

5837 [Pro3]-GIP (Rat) High affinity rat GIP partial agonist 1 mg

2257 GIP (1-39) GIP agonist; highly potent insulinotropic peptide 1 mg

2084 GIP (human) GIP agonist: potent insulinotropic gut hormone 1 mg

Antagonists 5838 [Pro3]-GIP (Mouse) GIP antagonist 1 mg

Glucagon Receptors

Antagonists 2216 des-His1-[Glu9]-Glucagon (1-29) amide

Glucagon receptor antagonist 1 mg

2311 L-168,049 Potent human glucagon receptor antagonist; orally active 10 mg

50 mg

Glucagon-Like Peptide 1 Receptors

Agonists 1933 Exendin-4 Potent GLP-1 agonist 1 mg

5374 GLP-1 (7-37) Endogenous bioactive GLP-1 receptor ligand 1 mg

1851 Glucagon-like peptide 1 (1-37) (human, rat)

Endogenous pancreatic peptide 1 mg

2082 Glucagon-like peptide 1 (7-36) amide (human, rat)

Potent insulinotropic peptide 1 mg

6517 Liraglutide Potent, long-acting GLP-1 agonist 1 mg

2094 Oxyntomodulin (porcine, bovine) GLP-1 receptor agonist; modulates feeding and metabolism 1 mg

Antagonists 2081 Exendin-3 (9-39) amide Potent GLP-1 antagonist 1 mg

3266 GLP-1 (9-36) amide GLP-1 antagonist; metabolite of GLP-1-(7-36) (Cat. No. 2082) 1 mg

6355 VU 0650991 Non-competitive GLP-1 antagonist; orally bioavailable and brain penetrant 10 mg

50 mg

Modulators 4778 BETP Positive allosteric modulator of GLP-1 receptors 10 mg

50 mg

Glucagon-Like Peptide 2 Receptors

Agonists 2258 GLP-2 (human) Endogenous GLP-2 agonist; displays intestinotrophic activity 1 mg

2259 GLP-2 (rat) Endogenous GLP-2 agonist; displays intestinotrophic activity 1 mg

Insulin and Insulin-like Receptors

Activators 1819 Demethylasterriquinone B1 Selective insulin RTK activator 5 mg

3435 Insulin (human) recombinant Endogenous peptide agonist; expressed in yeast 10 mg

Inhibitors 4774 BMS 536924 Dual IR/IGF1R inhibitor 10 mg

50 mg

5111 GSK 1838705 Potent IR and IGF1R inhibitor; also inhibits anaplastic lymphoma kinase (ALK) 10 mg

50 mg

2956 Picropodophyllotoxin Selective IGF1R inhibitor 10 mg

2768 PQ 401 IGF1R inhibitor 10 mg

50 mg

Others 5192 NBI 31772 High affinity insulin-like growth factor-I binding protein (IGFBP) inhibitor 10 mg

50 mg

Glucose RegulationGlucose homeostasis is vital for maintaining a sufficient level of glucose in the body, whilst preventing the serious clinical outcomes associated with hyperglycemia, as observed in diabetes. Regulatory peptides involved in glucose homeostasis, such as insulin and glucagon-like peptide 1 (GLP-1), and their receptors are key therapeutic targets in diabetes research.

Category Cat. No. Product Name Description Unit Size

Tocris Product Listing Series

16 |

Calcitonin Receptors

Agonists 6031 Calcitonin (human) Endogenous calcitonin agonist; inhibits bone resorption 500 µg

1159 Calcitonin (salmon) Endogenous calcitonin agonist; affects bone formation and resorption 200 µg

2550 SUN-B 8155 Non-peptide calcitonin (CT) receptor agonist 10 mg

50 mg

Mas-Related G Protein-Coupled Receptors

Agonists 1763 BAM (8-22) Potent MRGPRX1 agonist 1 mg

3374 Cortistatin 14 Endogenous neuropeptide; binds sst1 - sst5, ghrelin receptor and MRGPRX2 1 mg

6551 PAMP-12 (human, porcine) Potent MRGPRX2 agonist 1 mg

6552 PAMP-20 (human) MRGPRX2 agonist 1 mg

5473 PMX 53 MRGPRX2 agonist; also potent C5a receptor antagonist 1 mg

6351 (R)-ZINC 3573 MRGPRX2 agonist 5 mg

25 mg

Antagonists 6642 QWF MRGPRX2 antagonist; also NK1 antagonist 5 mg

Modulators 5738 ML 382 Positive allosteric modulator of MRGPRX1 receptors 10 mg

50 mg

Controls 6352 (S)-ZINC 3573 Negative control for (R)-ZINC 3573 (Cat. No. 6351) 5 mg

25 mg

Neuropeptide FF/AF Receptors

Agonists 1928 Neuropeptide AF (human) Endogenous NPFF1 and NPFF2 agonist; antiopioid neuropeptide and MRGPRA agonist

1 mg

3137 Neuropeptide FF Endogenous NPFF1 and NPFF2 agonist 1 mg

4683 RFRP 3 (human) NPFF1 agonist; GnIH homolog 1 mg

Antagonists 2707 BIBP 3226 trifluoroacetate Mixed NPY Y1 and NPFF antagonist 1 mg

10 mg

3672 RF 9 Selective NPFF1 and NPFF2 antagonist 1 mg

Ligands 1486 GR 231118 Binds to NPFF receptors; also potent NPY Y1 antagonist and Y4 agonist 500 µg

Other Peptide ReceptorsNumerous processes are influenced by peptide hormones, including calcium regulation (calcitonin and parathyroid hormone), uterine contraction (oxytocin) and nociception (neuropeptide FF). Regulation of calcium homeostasis is of particular importance in osteoporosis.

Cys-Tyr-Ile-Gln-Asn-Cys-Pro-Leu-Gly-NH2

Oxytocin (1910)Involved in uterine contraction and lactation

N

OMe

O

N

O

N

O O

O

L-371,257 (2410)Potent and selective oxytocin receptor antagonist

Et2N

O

OMe

H

N

N

Me

Me

SNC 80 (0764)Highly selective non-peptide δ agonist

HOHO

N

HO

N NH

S

NH

O

O

OHOHO

Naloxone fluorescein (6046)Fluorescent opioid antagonist; fluorescent-derivative

of naloxone (Cat. No. 0599)

Ala-Val-Ser-Glu-Ile-Gln-Leu-Met-His-Asn-Leu-Gly-Lys-His-Leu-Ala-Ser-Val-Glu-Arg-Met-Gln-Trp-Leu-Arg-Lys-Lys-Leu-Gln-Asp-Val-His-Asn-Phe

Parathyroid hormone (1-34) (rat) (6301)Parathyroid hormone (PTH) receptor agonist

Key Products for Oxytocin Receptors

Category Cat. No. Product Name Description Unit Size

PEPTIDE HORMONE RECEPTORS

www.tocris.com | 17

Opioid Receptors

Agonists 4335 AR-M 1000390 Low-internalizing δ agonist 10 mg

50 mg

2808 Buprenorphine NOP agonist; also displays mixed action at δ, κ and μ receptors 10 mg

50 mg

3790 DADLE Prototypical δ agonist 5 mg

1171 DAMGO Selective μ agonist 1 mg

1431 DPDPE Selective δ agonist 1 mg

3195 Dynorphin A Endogenous κ agonist 1 mg

3196 Dynorphin B Endogenous κ agonist 1 mg

1055 Endomorphin-1 Potent and selective μ agonist 5 mg

5158 Morphine Narcotic opioid analgesic 50 mg

1780 NNC 63-0532 Potent non-peptide NOP agonist; brain penetrant 10 mg

50 mg

0910 Nociceptin Endogenous NOP agonist 1 mg

0921 SB 205607 Selective, high affinity non-peptide δ1 agonist 10 mg

3240 SCH 221510 Potent and selective NOP agonist 10 mg

50 mg

0764 SNC 80 Highly selective non-peptide δ agonist 10 mg

50 mg

0495 (±)-U-50488 Selective κ agonist 25 mg

0496 (-)-U-50488 Selective κ agonist; more active enantiomer of (±)-U-50488 (Cat. No. 0495)

10 mg

50 mg

Antagonists 0347 nor-Binaltorphimine Selective κ antagonist 10 mg

50 mg

1560 CTAP Potent and selective μ antagonist 1 mg

1578 CTOP Potent and selective μ antagonist 1 mg

2601 Cyprodime Selective μ antagonist 10 mg

0794 DIPPA Selective and irreversible κ antagonist 10 mg

50 mg

0926 β-Funaltrexamine Irreversible and selective μ antagonist 10 mg

50 mg

2598 (±)-J 113397 Potent and selective NOP antagonist 10 mg

50 mg

6046 Naloxone fluorescein Fluorescent opioid antagonist; fluorescent-derivative of naloxone (Cat. No. 0599)

100 µg

0599 Naloxone Non-selective opioid antagonist 100 mg

0677 Naltrexone Non-selective opioid antagonist 100 mg

0892 Naltriben Standard δ2 selective antagonist 10 mg

50 mg

0740 Naltrindole Selective non-peptide δ antagonist 10 mg

50 mg

3573 SB 612111 Selective NOP antagonist 10 mg

50 mg

Modulators 5983 BMS 986187 Potent positive allosteric modulator of δ receptors 10 mg

50 mg

Oxytocin Receptors

Agonists 4852 Carbetocin Oxytocin agonist; analog of Oxytocin (Cat. No. 1910) 10 mg

1910 Oxytocin Oxytocin agonist; involved in uterine contraction and lactation 1 mg

4625 TC OT 39 Potent non-peptide oxytocin partial agonist; also V1a antagonist 10 mg

3933 WAY 267464 Potent non-peptide oxytocin agonist 10 mg

Antagonists 6332 Atosiban Potent oxytocin antagonist 10 mg

2641 L-368,899 Potent non-peptide oxytocin antagonist 1 mg

10 mg

2410 L-371,257 Potent and selective oxytocin antagonist 10 mg

Category Cat. No. Product Name Description Unit Size

Tocris Product Listing Series

18 |

PACAP Receptors

Agonists 1183 PACAP 1-27 Endogenous neuropeptide; potent stimulator of adenylyl cyclase 100 µg

1186 PACAP 1-38 Endogenous neuropeptide; potent stimulator of adenylyl cyclase 100 µg

Antagonists 6657 PA 8 PAC1 antagonist 10 mg

50 mg

3236 PACAP 6-38 Potent PAC1 antagonist 100 µg

Parathyroid Hormone Receptors

Agonists 5487 DPC AJ1951 Potent parathyroid hormone (PTH) receptor agonist 1 mg

6303 Parathyroid hormone (1-34) (bovine)

Parathyroid hormone (PTH) receptor agonist 1 mg

3011 Parathyroid hormone (1-34) (human)

Parathyroid hormone (PTH) receptor agonist 1 mg

6301 Parathyroid hormone (1-34) (rat) Parathyroid hormone (PTH) receptor agonist 1 mg

VIP Receptors

Agonists 2711 Bay 55-9837 Potent and selective VPAC2 agonist 1 mg

1911 VIP (human, rat, mouse, rabbit, canine, porcine)

Involved in neurotransmission and smooth muscle relaxation 1 mg

Antagonists 3054 [D-p-Cl-Phe6,Leu17]-VIP Selective VIP receptor antagonist 1 mg

1905 VIP (6-28) (human, rat, porcine, bovine)

VIP receptor antagonist 1 mg

Category Cat. No. Product Name Description Unit Size

Other Peptide Hormones – continued

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PEPTIDE HORMONE RECEPTORS

www.tocris.com | 19

Peptide Hormone ProcessingPeptide hormone signaling is modulated by various proteases that metabolize peptide hormones. Examples include: dipeptidyl peptidase IV, which degrades glucagon-like peptide 1 thereby curbing insulin secretion; and angiotensin-converting enzyme, which catalyzes the conversion of angiotensin I to angiotensin II.

Aminopeptidases

Inhibitors 1956 Bestatin Aminopeptidase inhibitor 10 mg

3595 CHR 2797 Aminopeptidase inhibitor 1 mg

10 mg

5627 HFI 142 Insulin-regulated aminopeptidase (IRAP) inhibitor 10 mg

50 mg

Angiotensin-Converting Enzyme

Inhibitors 2578 Benazepril Angiotensin-converting enzyme (ACE) inhibitor 50 mg

4455 Captopril ACE inhibitor; also inhibits LTA4 hydrolase 50 mg

4302 Perindopril Angiotensin-converting enzyme (ACE) inhibitor 50 mg

2931 Spinorphin Enkephalin-degrading and ACE inhibitor 1 mg

Ligand 6006 Acein High affinity angiotensin-converting enzyme (ACE) ligand 1 mg

3791 Hemopressin (human, mouse) Bioactive substrate for endopeptidase 24.15, neurolysin and ACE 1 mg

Chymase

Substrates 3841 RETF-4NA Selective chymase substrate 1 mg

Dipeptidyl Peptidase IV (DPP-IV)

Inhibitors 6019 Diprotin A Dipeptidyl peptidase IV (DPP-IV) inhibitor 10 mg

2783 DPPI 1c Dipeptidyl peptidase IV (DPP-IV) inhibitor 1 mg

10 mg

2790 K 579 Dipeptidyl peptidase IV (DPP-IV) inhibitor 10 mg

50 mg

3506 NVP DPP 728 Potent dipeptidyl peptidase IV (DPP-IV) inhibitor; orally active 10 mg

50 mg

4145 PK 44 Potent and selective dipeptidyl peptidase IV (DPP-IV) inhibitor 10 mg

6816 Sitagliptin Potent and selective DPP IV inhibitor 10 mg

50 mg

6507 Saxagliptin High affinity DPP-IV inhibitor; active in vivo 10 mg

50 mg

Endothelin-converting Enzyme

Inhibitors 2512 CGS 35066 Endothelin-converting enzyme (ECE) inhibitor 10 mg

6333 Phosphoramidon disodium salt Neutral endopeptidase and endothelin converting enzyme inhibitor 5 mg

Insulin-degrading Enzyme (IDE)

Inhibitors 5402 6bK Insulin degrading enzyme (IDE) inhibitor 1 mg

500 µg

Neurotensin-degrading Enzymes

Inhibitors 2575 JMV 390-1 Inhibits multiple neurotensin and neuromedin N degrading enzymes 1 mg

Renin

Inhibitors 5491 Aliskiren Potent renin inhibitor; antihypertensive 10 mg

50 mg

5563 VTP 27999 Highly potent and selective renin inhibitor 10 mg

Tripeptidyl Peptidase II

Inhibitors 1323 Butabindide High affinity CCK-inactivating serine protease inhibitor 10 mg

50 mg

Category Cat. No. Product Name Description Unit Size

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