Peptide Hormone Receptors
Products for:• Anterior Pituitary Regulation• Blood Pressure Regulation• Feeding and Appetite Regulation• Glucose Regulation• Other Peptide Hormones• Peptide Hormone Processing
Oriental Fire-bellied ToadBombina orientalisA source of Bombesin
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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.Receptor... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 5
Neurotensin.(NT).Receptors... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 5
Somatostatin.(sst).Receptors... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 5
Thyrotropin-releasing.Hormone.(TRH).Receptors... . . . . . . . 5
Blood Pressure Regulation.. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . .6
Angiotensin.(AT).Receptors... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 6
Apelin.(APJ).Receptors... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 7
Bradykinin.Receptors... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 7
Calcitonin.Gene-related.Peptide.(CGRP).Receptor... . . . . . 7
Endothelin.(ET).Receptors... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 7
Natriuretic.Peptide.Receptors.(NPR).... . . . . . . . . . . . . . . . . . . . . . . . . . . . 7
Tachykinin.(NK).Receptors... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 8
Urotensin-II.(UT).Receptor... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 9
Vasopressin.Receptors... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 9
Feeding and Appetite Regulation.. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 10
Bombesin.(BB).Receptors... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 10
CART.... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 10
Cholecystokinin.(CCK).Receptors... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 10
Galanin.(GAL).Receptors... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 11
Ghrelin.&.Ghrelin-related.Receptors... . . . . . . . . . . . . . . . . . . . . . . . . . . . 11
GPR103.(QRFP.Receptor)... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 12
Leptin.Receptors... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 12
Melanin-concentrating.Hormone.(MCH).Receptors... . . 12
Melanocortin.(MC).Receptors... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 12
Motilin.Receptors... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 12
Neuromedin.U.(NMU).Receptors... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 12
Neuropeptide.B/W.(NPBW).Receptors... . . . . . . . . . . . . . . . . . . . . . . . 12
Neuropeptide.S.Receptor... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 13
Neuropeptide.Y.(NPY).Receptors... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 13
Opioid.Receptors... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 14
Orexin.Receptors... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 14
VIP.and.PACAP.Receptors... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 14
Glucose Regulation.. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 15
Amylin.Receptor... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 15
Gastric.Inhibitory.Polypeptide.(GIP).Receptor... . . . . . . . . . . . 15
Glucagon.Receptor... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 15
Glucagon-like.Peptide.1.(GLP-1).Receptor... . . . . . . . . . . . . . . . . 15
Glucagon-like.Peptide.2.(GLP-2).Receptor... . . . . . . . . . . . . . . . . 15
Insulin.Receptor... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 15
Insulin-like.Growth.Factor.1.Receptor.(IGF1R).... . . . . . . . . 15
Other Peptide Hormones.. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 16
Calcitonin.Receptor... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 16
Neuropeptide.FF/AF.(NPFF).Receptors... . . . . . . . . . . . . . . . . . . . . . . 16
Oxytocin.Receptor... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 16
Parathyroid.Hormone.Receptors... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 16
Peptide Hormone Processing.. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 17
Angiotensin-converting.Enzyme.(ACE).... . . . . . . . . . . . . . . . . . . . . . . 17
Chymase.... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 17
Dipeptidyl.Peptidase.IV.(DPP-IV)... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 17
Endothelin-converting.Enzyme.(ECE).... . . . . . . . . . . . . . . . . . . . . . . . . 17
Neurotensin-degrading.Enzymes.... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 17
Tripeptidyl.Peptidase.II... . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 17
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 ReceptorTRH Receptors
Heart, Arteries and KidneysBlood Pressure RegulationAngiotensin ReceptorsApelin ReceptorsBradykinin ReceptorsCGRP ReceptorEndothelin ReceptorsNatriuretic Peptide ReceptorsTachykinin ReceptorsUrotensin-II ReceptorVasopressin Receptors
Liver and PancreasGlucose RegulationAmylin ReceptorGIP ReceptorGlucagon-like Peptide 1 ReceptorGlucagon-like Peptide 2 ReceptorInsulin ReceptorInsulin-like Growth Factor Receptor
Stomach and GutAppetite & Feeding RegulationBombesin ReceptorsCARTCCK ReceptorsGalanin ReceptorsGhrelin & Ghrelin-related ReceptorsGPR103 (QRFP Receptor)Leptin ReceptorsMCH ReceptorsMelanocortin ReceptorsMotilin ReceptorNeuromedin U ReceptorsNeuropeptide B/W ReceptorsNeuropeptide S ReceptorNeuropeptide Y ReceptorsOpioid ReceptorsOrexin ReceptorVIP and PACAP 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).
Highly Potent Neurotensin Receptor Antagonist
SR 142948 Cat. No. 2309
SR.142948.is.a.potent.non-peptide.neurotensin.(NT).receptor.antagonist.that.binds.with.high.affinity.(IC50.=.0.32.–.3.96.nM;.Ki.<.10.nM)..The.compound.attenuates.amphetamine-induced.hyperactivity.and.is.orally.active.in vivo.
N
O
N
N
N
OMe
MeO
NHO CO2H
Selective, Non-peptide CRF1 Antagonist
CP 154526 Cat. No. 2779
CP.154526.is.a.selective,.non-peptide.CRF1.receptor.antagonist.(Ki.values.are.2.7.and.>10000.nM.for.CRF1.and.CRF2.receptors.respectively)..The.compound.blocks.CRF-induced.adenylate.cyclase.activation.(Ki.=.3.7.nM).and.attenuates.activation.of.the.HPA.axis.by.CRF..CP.154526.displays.anxiolytic-like.activity.in.the.rat.elevated.plus-maze.test,.and.is.brain.penetrant.
(Sold for research purposes under agreement from Pfizer Inc.)
N N
NN
Category Cat. No. Product Name Description Unit Size USD
Corticotropin-releasing Factor (CRF) Receptors
Agonists 1151 CrF (human, rat) Stimulates ACTH release 200 µg 155
1608 Stressin i CrF1 agonist 500 µg 365
1604 Urocortin (human) endogenous CrF agonist 1 mg 415
1605 Urocortin (rat) endogenous CrF agonist 1 mg 415
Antagonists 2778 Antalarmin CrF1 antagonist 10 mg
50 mg
195
819
2071 Antisauvagine-30 Potent, selective and competitive CrF2 antagonist 1 mg 389
1606 Astressin Potent CrF receptor antagonist 500 µg 315
2391 Astressin 2B Selective CrF2 antagonist 500 µg 385
2779 CP 154526 Selective, non-peptide CrF1 antagonist 10 mg
50 mg
195
819
3212 CP 376395 Potent and selective CrF1 antagonist 10 mg
50 mg
185
779
1184 α-helical CrF 9-41 CrF receptor antagonist 500 µg 255
2070 K 41498 Highly selective and potent CrF2 antagonist 1 mg 389
1591 nBi 27914 Selective non-peptide CrF1 antagonist 10 mg
50 mg
149
629
3100 nBi 35965 Potent and selective CrF1 antagonist 10 mg
50 mg
199
839
3294 Sn 003 Potent and selective CrF1 antagonist 10 mg 189
Other 1607 CrF (6-33) CrF binding protein inhibitor 1 mg 335
Gonadotropin-releasing Hormone (GnRH) Receptors
Agonists 3592 Goserelin acetate GnrH receptor agonist 10 mg 155
2873 Leuprolide GnrH receptor agonist 1 mg 75
2544 nafarelin GnrH receptor agonist 1 mg 129
Antagonists 2730 AG 045572 Selective GnrH receptor antagonist 1 mg
10 mg
105
219
3536 Cetrorelix acetate Potent GnrH antagonist 1 mg 195
2519 T 98475 GnrH receptor antagonist 1 mg 219
PePTide Hormone reCePTorS
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D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-ol
Octreotide (1818)sst2, sst3 and sst5 agonist
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
Key Products for Anterior Pituitary Regulation
Anterior Pituitary regulation – continued
Category Cat. No. Product Name Description Unit Size USD
Kisspeptin Receptor
Agonists 2570 Kisspeptin 10 (human) endogenous ligand for KiSS1 receptor 1 mg 279
4243 Kisspeptin 10 (rat) endogenous ligand for KiSS1 receptor 1 mg 159
Antagonists 3881 Kisspeptin 234 KiSS1/GPr54 antagonist; kisspeptin 10 (Cat. no. 2570) analog 1 mg 129
Neurotensin (NT) Receptors
Agonists 1998 JmV 449 Potent neurotensin receptor agonist 1 mg 105
1909 neurotensin endogenous neurotransmitter and endocrine modulator 1 mg 75
Antagonists 2309 Sr 142948 Highly potent neurotensin receptor antagonist 1 mg
10 mg
125
265
3721 Sr 48692 Selective non-peptide nTS1 antagonist 10 mg
50 mg
249
1049
Somatostatin (sst) Receptors
Agonists 2842 Bim 23052 sst5 agonist 1 mg 195
2454 CH 275 Potent and selective sst1 receptor agonist 1 mg 249
2444 (1R,1ʹS,3ʹR/1R,1ʹR,3ʹS)-L-054,264 Potent and selective sst2 agonist 1 mg
10 mg
115
239
1979 L-803,087 Potent and selective sst4 agonist 10 mg 275
1980 L-817,818 Potent and selective sst5 agonist 10 mg 275
2440 nnC 26-9100 Selective sst4 agonist 10 mg 219
1818 octreotide sst2, sst3 and sst5 agonist 1 mg 255
1157 Somatostatin endogenous sst agonist; influences growth hormone release 1 mg 105
1165 Somatostatin 1-28 sst receptor agonist 500 µg 285
4639 TT 232 sst1/sst4 receptor agonist 1 mg 195
Antagonists 3493 Cyclosomatostatin non-selective sst receptor antagonist 1 mg 169
1843 CYn 154806 Selective sst2 antagonist 1 mg 235
Ligands 1844 Bim 23056 Somatostatin receptor ligand 1 mg 219
Other 3374 Cortistatin 14 endogenous neuropeptide; binds sst1 - sst5 and GHS-r1a 1 mg 205
Thyrotropin-releasing Hormone (TRH) Receptors
Agonists 2672 Taltirelin Synthetic thyrotropin-releasing hormone analog 1 mg
10 mg
105
219
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Blood Pressure 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.
N
N
N
NMe2
Me
Ph2HC
O
HO2C
PD 123319 (1361)Potent, selective non-peptide AT2 antagonist
N O
N
Et
Et
N
N N
NH
ZD 7155 (1211)Selective non-peptide AT1 antagonist
pGlu-Arg-Pro-Arg-Leu-Ser-His-Lys-Gly-Pro-Met-Pro-Phe
[Pyr1]-Apelin-13 (2420)Potent peptide agonist for apelin receptor
O
O
S
O
OO2N
N
N
ML 221 (4748)Apelin receptor antagonist
Key Products for Angiotensin and Apelin Receptors
Category Cat. No. Product Name Description Unit Size USD
Angiotensin (AT) Receptors
Agonists 1562 Angiotensin (1-7) Vasorelaxant peptide 1 mg 65
1563 Angiotensin i (human, mouse, rat) endogenous precursor to angiotensin ii (Cat. no. 1158) 1 mg 75
1158 Angiotensin ii Potent vasoconstrictor peptide 5 mg 115
Antagonists 4553 Azilsartan Potent AT1 receptor inverse agonist; antihypertensive 10 mg
50 mg
165
695
4792 Candesartan cilexetil Prodrug of candesartan (Cat. no. 4791), an AT1 receptor antagonist
10 mg
50 mg
69
295
1849 emd 66684 Potent, selective non-peptide AT1 antagonist 10 mg
50 mg
195
819
4696 eprosartan Potent and selective AT1 receptor antagonist 10 mg
50 mg
59
249
3798 Losartan Selective, non-peptide AT1 antagonist 50 mg 105
4616 olmesartan Potent AT1 antagonist 50 mg 105
1361 Pd 123319 Potent, selective non-peptide AT2 antagonist 10 mg
50 mg
195
819
4216 Valsartan High affinity, selective AT1 antagonist 10 mg
50 mg
189
795
1211 Zd 7155 Selective non-peptide AT1 antagonist 10 mg
50 mg
169
715
Ligands 2569 CGP 42112 Selective, high affinity AT2 ligand 1 mg 169
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Blood Pressure regulation – continued
Category Cat. No. Product Name Description Unit Size USD
Apelin (APJ) Receptors
Agonists 2420 [Pyr1]-Apelin-13 Potent peptide agonist for APJ receptor 1 mg 169
3007 Apelin-17 (human, bovine) endogenous APJ receptor agonist 1 mg 235
2426 Apelin-36 (human) endogenous APJ receptor agonist 1 mg 415
2427 Apelin-36 (rat, mouse) endogenous APJ receptor agonist 1 mg 415
Antagonists 4748 mL 221 APJ receptor antagonist 10 mg
50 mg
185
779
Bradykinin Receptors
Agonists 3004 Bradykinin endogenous agonist at bradykinin receptors (B2 > B1) 5 mg 79
3005 [des-Arg9]-Bradykinin Bradykinin receptor agonist (B1 > B2) 5 mg 59
3229 [Phe8Ψ(CH-nH)Arg9]-Bradykinin Selective B2 agonist 1 mg 205
3227 Lys-Bradykinin Potent bradykinin receptor agonist (B2 > B1) 1 mg 75
3225 Lys-[des-Arg9]Bradykinin Selective B1 agonist 1 mg 75
3230 Sar-[d-Phe8]-des-Arg9-Bradykinin Potent and selective B1 agonist 1 mg 195
Antagonists 3014 Hoe 140 Potent and selective B2 antagonist 500 µg 195
3978 men 11270 Selective B2 antagonist; analog of Hoe 140 (Cat. no. 3014) 500 µg 325
1697 noscapine Bradykinin antagonist. Also tubulin inhibitor 100 mg 95
3407 r 715 Potent and selective B1 antagonist 1 mg 205
3226 r 892 Potent and selective B1 antagonist 1 mg 205
1057 Win 64338 Bradykinin B2 antagonist 10 mg
50 mg
185
779
Other 2370 Bombinakinin-GAP Bioactive, bradykinin-related peptide 1 mg 205
Calcitonin Gene-related Peptide (CGRP) Receptor
Agonists 3012 α-CGrP (human) CGrP receptor agonist 1 mg 405
Antagonists 4561 BiBn 4096 Potent and selective CGrP receptor antagonist 10 mg 285
1181 CGrP 8-37 (human) CGrP1 receptor antagonist 500 µg 285
1169 CGrP 8-37 (rat) CGrP1 receptor antagonist 500 µg 295
4314 SB 268262 Selective non-peptide CGrP1 antagonist 10 mg
50 mg
219
925
Endothelin (ET) Receptors
Agonists 1189 BQ-3020 Selective eTB agonist 500 µg 219
1160 endothelin 1 (human, porcine) Potent vasoconstrictor peptide 100 µg 179
1164 endothelin 2 (human) eTA/eTB agonist 100 µg 179
1162 endothelin 3 (human, rat) Potent vasoconstrictor 100 µg 179
1175 Sarafotoxin S6c Selective eTB agonist 100 µg 179
Antagonists 1441 BmS 182874 Highly selective, orally active non-peptide eTA antagonist 10 mg
50 mg
195
819
1188 BQ-123 Selective eTA antagonist 500 µg 169
1500 BQ 788 Selective eTB antagonist 1 mg 305
1210 Fr 139317 Highly potent, selective eTA antagonist 10 mg
50 mg
215
905
1838 irL-2500 Potent eTB antagonist 10 mg 245
Natriuretic Peptide Receptors (NPR)
Agonists 1906 Atrial natriuretic factor (1-28) (human, porcine)
endogenous peptide regulating blood pressure 1 mg 315
1912 Atrial natriuretic factor (1-28) (rat) endogenous peptide regulating blood pressure 1 mg 295
3522 Brain natriuretic peptide (1-32) (human)
endogenous peptide agonist at AnP receptor A (nPr1) 1 mg 375
3520 C-type natriuretic peptide (1-22) (human, rat, swine)
endogenous peptide agonist at nPr2 500 µg 185
Tocris Product Listing Series
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Potent and Selective CGRP Receptor Antagonist
BIBN 4096 Cat. No. 4561
BIBN.4096.is.a.potent.and.selective.CGRP.receptor.antagonist.(IC50.values.are.0.03.and.6.4.nM.for.human.and.rat.CGRP.receptors.respectively)..The.compound.displays.high.affinity.for.human.CGRP.receptors.(Ki.=.14.4.pM).but.exhibits.no.significant.affinity.against.a.panel.of.75.other.receptors..
NHN
N
HNO
O
HN
N N NO O
NH2
Br
Br
HO
Potent and Selective B2 Antagonist
HOE 140 Cat. No. 3014
HOE.140.is.a.potent.and.selective.bradykinin.B2.receptor.antagonist.(pA2.=.9.04)..The.compound.also.inhibits.aminopeptidase.N.(Ki.=.9.1.µM).
D-Arg-Arg-Pro-Hyp-Gly-Thi-Ser-D-Tic-Oic-Arg
Category Cat. No. Product Name Description Unit Size USD
Tachykinin (NK) Receptors
Agonists 1668 Gr 64349 Potent, selective nK2 agonist 1 mg 345
1669 Gr 73632 Potent, selective nK1 agonist 1 mg 315
1535 Hemokinin 1 (mouse) endogenous, high affinity, selective nK1 agonist 1 mg 205
1640 [bAla8]-neurokinin A(4-10) nK2 agonist 1 mg 205
1152 neurokinin A (porcine) endogenous tachykinin peptide 1 mg 145
1582 neurokinin B (human, porcine) endogenous tachykinin peptide 1 mg 169
3228 [Lys5,meLeu9,nle10]-nKA(4-10) Selective nK2 agonist 1 mg 195
1068 Senktide Tachykinin nK3 agonist 500 µg 115
1178 [Sar9,met(o2)11]-Substance P Potent, selective nK1 agonist 1 mg 145
1156 Substance P Sensory neuropeptide, inflammatory mediator 5 mg 139
Antagonists 1954 Antagonist G Broad spectrum neuropeptide receptor antagonist 1 mg 169
2893 CP 96345 Potent and selective nK1 antagonist 10 mg
50 mg
199
839
2400 FK 888 High affinity nK1 receptor antagonist 10 mg 275
1274 Gr 159897 non-peptide, potent nK2 antagonist 10 mg
50 mg
195
819
1667 Gr 94800 Potent, selective nK2 antagonist 1 mg 399
0868 L-732,138 Potent, selective nK1 antagonist 10 mg
50 mg
89
339
1145 L-733,060 Potent nK1 antagonist 10 mg
50 mg
195
819
4013 L 760735 High affinity nK1 receptor antagonist 10 mg
50 mg
219
925
1635 rP 67580 Potent and selective nK1 antagonist 10 mg
50 mg
195
819
1376 SB 218795 Potent, selective non-peptide nK3 antagonist 10 mg
50 mg
195
819
1393 SB 222200 Potent, selective non-peptide nK3 antagonist. Brain penetrant 10 mg
50 mg
185
779
4012 Sr 140333 Potent nK1 receptor antagonist 10 mg
50 mg
249
1049
1946 [d-Arg1,d-Phe5,d-Trp7,9,Leu11]-Substance P
Substance P analog and broad spectrum neuropeptide receptor antagonist/inverse agonist
1 mg 139
PePTide Hormone reCePTorS
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Blood Pressure regulation – continued
Cys-Ser-Cys-Ser-Ser-Leu-Met-Asp-Lys-Glu-
Cys-Val-Tyr-Phe-Cys-His-Leu-Asp-lle-Ile-Trp
Endothelin 1 (human, porcine) (1160)Potent vasoconstrictor peptide
NH
HN
O
N
OO NH
Me3C
Me
Me
N
OMeO
NaO2C
BQ 788 (1500)Selective ETB antagonist
Ser-Leu-Arg-Arg-Ser-Ser-Cys-Phe-Gly-Gly-Arg-Met-Asp-Arg-Ile-Gly-Ala-Gln-Ser-Gly-
Leu-Gly-Cys-Asn-Ser-Phe-Arg-Tyr
Atrial natriuretic factor (1-28) (human, porcine) (1906)Endogenous peptide regulating blood pressure
Ser-Pro-Lys-Met-Val-Gln-Gly-Ser-Gly-Cys-Phe-Gly-Arg-Lys-Met-Asp-Arg-Ile-Ser-Ser-
Ser-Ser-Gly-Lys-Gly-Cys-Lys-Val-Leu-Arg-Arg-His
Brain natriuretic peptide (1-32) (human) (3522)Endogenous peptide agonist at ANP receptor A (NPR1)
Key Products for Endothelin and Natriuretic Peptide Receptors
Arg-Pro-Lys-Pro-Gln-Gln-Phe-Phe-Gly-Leu-Met-NH2
Substance P (1156)Sensory neuropeptide, inflammatory mediator
NH
O
CF3
CF3
L-733,060 (1145)Potent NK1 antagonist
Cys-Tyr-Phe-Gln-Asn-Cys-Pro-Arg-Gly-NH2
[Arg8]-Vasopressin (2935)Antidiuretic hormone
OMe
OMe
SN
O
O
Cl OH O
N
O NH2
Cl
SR 49059 (2310)Selective, orally active vasopressin
V1A receptor antagonist
Key Products for Tachykinin and Vasopressin Receptors
Category Cat. No. Product Name Description Unit Size USD
Urotensin-II (UT) Receptor
Agonists 1642 Urotensin-ii (human) endogenous vasoactive agonist for the urotensin-ii receptor 1 mg 255
Antagonists 4670 SB 611812 Urotensin-ii receptor antagonist; attenuates cardiac dysfunction 10 mg
50 mg
185
779
3571 SB 657510 Selective urotensin-ii receptor antagonist 10 mg
50 mg
189
795
2529 UFP 803 Urotensin-ii receptor antagonist 1 mg 205
3162 [orn5]-UrP Urotensin-ii receptor antagonist 1 mg 185
Vasopressin Receptors
Agonists 3396 desmopressin Synthetic vasopressin analog; V1B and V2 agonist 1 mg 105
2935 [Arg8]-Vasopressin Antidiuretic hormone 1 mg 75
3127 d[Leu4,Lys8]-VP Selective V1B agonist 1 mg 285
Antagonists 3924 oPC 21268 orally active vasopressin V1 antagonist 10 mg
50 mg
219
925
2310 Sr 49059 Selective, orally active vasopressin V1A receptor antagonist 10 mg 315
3377 (d(CH2)51,Tyr(me)2,Arg8)-
VasopressinSelective vasopressin V1A antagonist 1 mg 129
Tocris Product Listing Series
10 |
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.
HN NH
O
HN O
O
NHO
HO2C N
O
Me
NH2
O
t-BuHN O NH
Me
A-71623 (2411)Potent and selective CCK1 agonist;
suppresses feeding
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
His-D-Trp-D-Lys-Trp-D-Phe-Lys-NH2
[D-Lys3]-GHRP-6 (1922)Ghrelin receptor antagonist
N
N
O
O
N
F
YIL 781 (3959)Ghrelin receptor antagonist
Key Products for CCK, Galanin and Ghrelin Receptors
Category Cat. No. Product Name Description Unit Size USD
Bombesin (BB) Receptors
Agonists 2716 Bim 187 Bombesin/GrP receptor agonist 1 mg 185
1149 Bombesin Bombesin receptor agonist; involved in gastrointestinal tract function
1 mg 105
1789 GrP (human) endogenous GrP receptor agonist 1 mg 255
1788 GrP (porcine) endogenous GrP receptor agonist 1 mg 219
1908 neuromedin B (porcine) mammalian bombesin-like peptide 1 mg 129
Antagonists 2717 Bim 189 Bombesin receptor antagonist 1 mg 185
3237 Bim 23042 Selective BB1 receptor antagonist 1 mg 129
2602 Pd 176252 BB2 and BB1 receptor antagonist 10 mg 265
CART
Other 3339 CArT (62-76) (rat, human) neuromodulating neuropeptide fragment; inhibits food intake in vivo
1 mg 195
3338 CArT (55-102) (human) neuromodulatory neuropeptide fragment; satiety factor 100 µg 229
3337 CArT (55-102) (rat) neuromodulatory neuropeptide fragment; satiety factor 100 µg 259
Cholecystokinin (CCK) Receptors
Agonists 2411 A-71623 Potent and selective CCK1 agonist. Suppresses feeding 1 mg 259
1150 CCK octapeptide, non-sulfated non-sulfated form of CCK octapeptide (Cat. no. 1166) 1 mg 129
1166 CCK octapeptide, sulfated C-terminal octapeptide of CCK 1 mg 255
3006 Gastrin i (human) Selective CCK2 agonist 1 mg 285
Antagonists 2607 Ci 988 Potent and selective CCK2 antagonist 10 mg
50 mg
265
1115
2304 devazepide Selective, orally active CCK1 receptor antagonist 10 mg
50 mg
229
965
2767 L-365,260 Selective CCK2 antagonist 10 mg
50 mg
219
925
1524 LY 288513 Selective CCK2 antagonist 10 mg
50 mg
275
1155
PePTide Hormone reCePTorS
www.tocris.com | 11
Feeding and Appetite regulation – continued
Standard k Selective Antagonist
nor -Binaltorphimine Cat. No. 0347
nor-Binaltorphimine.is.a.selective.k.opioid.receptor.antagonist.that.reduces.food.intake.induced.by.food.deprivation.and.opioid.receptor.agonists..The.compound.reduces.meal.size.and.frequency,.increases.energy.expenditure.and.improves.satiation.in.obese.Zucker.rats.
(Sold with the permission of the University of Minnesota)
OO NH OH
HON
OHN
HO
Highly Potent and Selective OX2 Antagonist
EMPA Cat. No. 4558
EMPA.is.a.highly.potent,.selective.OX2.receptor.antagonist.(IC50.values.are.2.3.and.1900.nM.for.OX2.and.OX1.respectively)..The.compound.displays.negligible.or.no.inhibition.of.a.panel.of.80.receptors..EMPA.blocks.orexin-B.and.orexin-A-invoked.calcium.mobilization.in.hOX2-expressing.CHO.cells.(IC50.values.are.7.9.and.8.8.nM.respectively);.it.also.reverses.orexin-B-induced.hyperlocomotion.in.mice..EMPA.is.brain.penetrant.
N
N
O
NS
N
OMe
O O
Category Cat. No. Product Name Description Unit Size USD
Antagonists 2608 Pd 135158 Potent and selective CCK2 antagonist 10 mg
50 mg
249
1049
1478 Proglumide non-selective CCK antagonist; orally active 50 mg 59
2190 Sr 27897 Potent and selective CCK1 antagonist 10 mg
50 mg
195
819
1408 Ym 022 Highly potent, selective non-peptide CCK2 antagonist 10 mg
50 mg
185
779
Galanin (GAL) Receptors
Agonists 2699 Ar-m 1896 GAL2 agonist 1 mg 249
2696 Galanin (1-29) (rat, mouse) non-selective galanin receptor agonist 1 mg 205
1179 Galanin (1-30) (human) endogenous galanin receptor agonist 200 µg 185
1451 Galanin (2-29) (rat) Selective GAL2 peptide agonist 1 mg 399
2085 Galnon non-selective galanin receptor agonist 10 mg 129
3629 m 1145 Potent and selective GAL2 agonist 500 µg 295
2697 m617 Selective GAL1 agonist 1 mg 285
Antagonists 3425 m40 Potent, non-selective galanin receptor antagonist 1 mg 195
2698 m871 Selective GAL2 antagonist 1 mg 285
Ghrelin & Ghrelin-related Receptors
Agonists 1463 Ghrelin (human) endogenous ghrelin receptor agonist 1 mg 389
1465 Ghrelin (rat) endogenous ghrelin receptor agonist 1 mg 425
2261 L-692,585 Potent, non-peptide ghrelin receptor agonist 10 mg 265
2308 Tabimorelin Potent, orally active ghrelin receptor agonist 10 mg 315
Antagonists 3033 Cortistatin-8 Ghrelin receptor antagonist 1 mg 195
1922 [d-Lys3]-GHrP-6 Ghrelin receptor antagonist 5 mg 129
1946 [d-Arg1,d-Phe5,d-Trp7,9,Leu11]-Substance P
Potent ghrelin receptor full inverse agonist. Also antagonist at other neuropeptide receptors
1 mg 139
3959 YiL 781 Ghrelin receptor antagonist 10 mg
50 mg
205
865
Other 3374 Cortistatin 14 endogenous neuropeptide; binds ghrelin receptor and sst1 - sst5 1 mg 205
2260 [des-octanoyl]-Ghrelin (human) major circulating form of ghrelin; devoid of activity at ghrelin receptor but is active in vivo
1 mg 219
2951 [des-octanoyl]-Ghrelin (rat) major circulating form of ghrelin; devoid of activity at ghrelin receptor
1 mg 255
2445 obestatin (rat) endogenous anorexigenic peptide 1mg 75
Tocris Product Listing Series
12 |
Tyr-Val-Met-Gly-His-Phe-Arg-D-Trp-Asp-Arg-Phe-Gly
[D-Trp8]-γ-MSH (4272)Selective MC3 receptor agonist
Ac-Cys-Glu-His-D-2-Nal-Arg-Trp-Gly-Cys-Pro-Pro-Lys-Asp-NH2
HS 014 (1831)Selective MC4 receptor antagonist
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
NNH
ON
OMe
OMe
TCS OX2 29 (3371)Potent and selective OX2 antagonist
Key Products for Melanocortin and Orexin Receptors
Category Cat. No. Product Name Description Unit Size USD
GPR103 (QRFP Receptor)
Ligands 4402 26rFa Ligand of GPr103; orexigenic neuropeptide 1 mg 195
Leptin Receptors
Other 2985 LeP (116-130) (mouse) Synthetic leptin peptide fragment 1 mg 205
Melanin-concentrating Hormone (MCH) Receptors
Agonists 3434 [Ala17]-mCH Potent, mCH receptor agonist 1 mg 219
3806 mCH (human, mouse, rat) Potent endogenous mCH agonist 100 µg 79
Antagonists 3359 ATC 0065 Potent and selective mCH1 antagonist 10 mg
50 mg
199
839
3346 ATC 0175 mCH1 antagonist; also 5-HT2B antagonist and 5-HT1A partial agonist
10 mg
50 mg
199
839
4242 GW 803430 mCH1 antagonist 10 mg
50 mg
219
925
3347 SnAP 94847 Potent and selective mCH1 antagonist 10 mg
50 mg
195
819
4365 TC-mCH 7c Selective mCH1 antagonist 10 mg 249
Melanocortin (MC) Receptors
Agonists 3492 ACTH (1-39) Potent endogenous mC2 agonist 1 mg 335
4053 BmS 470539 Potent, selective mC1 receptor agonist 10 mg
50 mg
229
965
2566 melanotan ii High affinity melanocortin receptor agonist 1 mg 139
2584 α-mSH endogenous melanocortin receptor agonist 1 mg 75
3013 [nle4,d-Phe7]-α-mSH melanocortin receptor agonist 1 mg 159
4272 [d-Trp8]-γ-mSH Selective mC3 receptor agonist 1 mg 159
3032 THiQ Potent and selective mC4 receptor agonist 1 mg 219
Antagonists 1831 HS 014 Selective mC4 receptor antagonist 1 mg 305
1832 HS 024 Highly potent mC4 receptor antagonist 1 mg 305
3438 mCL 0020 Selective mC4 receptor antagonist 1 mg 205
Other 3420 SHU 9119 mC3 and mC4 antagonist, mC5 partial agonist 1 mg 129
Motilin Receptors
Other 2264 motilin (human, porcine) endogenous peptide regulator of gastrointestinal motility 1 mg 285
Neuromedin U (NMU) Receptors
Agonists 3648 neuromedin S (rat) Potent, endogenous nmU1 and nmU2 agonist 500 µg 295
1917 neuromedin U (rat) endogenous modulator of blood pressure and flow, gut ion transport, feeding and body temperature
1 mg 205
Neuropeptide B/W (NPBW) Receptors
Agonists 3009 neuropeptide W-23 (human) endogenous nPBW1 and nPBW2 receptor agonist 1mg 255
PePTide Hormone reCePTorS
www.tocris.com | 13
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
Category Cat. No. Product Name Description Unit Size USD
Neuropeptide S Receptor
Antagonists 4510 SHA 68 Selective neuropeptide S receptor antagonist 10 mg
50 mg
185
779
Neuropeptide Y (NPY) Receptors
Agonists 2035 BWX 46 Highly selective nPY Y5 agonist 1 mg 219
1177 neuropeptide Y 13-36 (porcine) nPY Y2 receptor agonist 500 µg 195
1176 [Leu31,Pro34]-neuropeptide Y (human, rat)
nPY Y1 receptor agonist 200 µg 139
1153 neuropeptide Y (human, rat) influences feeding and sexual behavior 200 µg 139
1168 [Leu31,Pro34]-neuropeptide Y (porcine)
nPY Y1 receptor agonist 200 µg 169
1173 neuropeptide Y (porcine) influences feeding and sexual behavior 200 µg 185
1154 Pancreatic Polypeptide (human) nPY Y4 agonist; involved in gastrointestinal tract function 200 µg 169
1365 [cPP1-7,nPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide
Potent, selective nPY Y5 agonist 1 mg 435
1618 Peptide YY (3-36) Selective nPY Y2 receptor agonist 500 µg 185
Antagonists 2412 BiBo 3304 Highly selective nPY Y1 receptor antagonist 10 mg
50 mg
289
1215
2707 BiBP 3226 mixed nPY Y1 and nPFF receptor antagonist 1 mg
10 mg
129
275
1700 Biie 0246 Potent, selective non-peptide nPY Y2 receptor antagonist 1 mg
10 mg
145
305
3242 BmS 193885 Potent, competitive nPY Y1 receptor antagonist 10 mg
50 mg
229
965
2199 CGP 71683 Highly selective and potent non-peptide nPY Y5 receptor antagonist
10 mg
50 mg
195
819
4606 CYm 9484 Potent nPY Y2 receptor antagonist 10 mg
50 mg
185
779
4018 JnJ 5207787 Selective nPY Y2 receptor antagonist 10 mg
50 mg
245
1029
1382 L-152,804 Potent, selective non-peptide nPY Y5 receptor antagonist 10 mg
50 mg
195
819
3562 LU AA33810 Potent nPY Y5 receptor antagonist 10 mg
50 mg
155
655
3677 nPY 5rA972 Potent and selective nPY Y5 antagonist 10 mg
50 mg
185
779
2200 Pd 160170 Selective non-peptide nPY Y1 receptor antagonist 10 mg
50 mg
165
695
3898 SF 11 nPY Y2 receptor antagonist 10 mg
50 mg
195
819
Tocris Product Listing Series
14 |
Feeding and Appetite regulation – continued
Category Cat. No. Product Name Description Unit Size USD
Opioid Receptors
Agonists 4335 Ar-m 1000390 Low-internalizing δ opioid receptor agonist 10 mg
50 mg
165
695
3790 dAdLe Prototypical δ agonist 5 mg 95
1171 dAmGo Selective µ agonist 1 mg 75
4591 deltorphin 1 Potent δ agonist 1 mg 95
1431 dPdPe Selective δ agonist 1 mg 115
3195 dynorphin A endogenous k agonist 1 mg 205
3196 dynorphin B endogenous k agonist 1 mg 205
1055 endomorphin-1 Potent and selective µ agonist 5 mg 115
0910 nociceptin endogenous noP agonist 1 mg 139
3240 SCH 221510 Potent and selective noP agonist 10 mg
50 mg
195
819
0764 SnC 80 Highly selective, non-peptide δ agonist 10 mg
50 mg
195
819
Antagonists 0347 nor-Binaltorphimine Standard k-selective antagonist 10 mg
50 mg
155
655
0740 naltrindole δ-selective non-peptide antagonist 10 mg
50 mg
135
559
Orexin Receptors
Agonists 1455 orexin A (human, rat, mouse) endogenous agonist at oX1 and oX2 500 µg 465
1456 orexin B (human) endogenous agonist at oX1 and oX2 500 µg 275
2142 [Ala11,d-Leu15]-orexin B Potent, selective oX2 receptor agonist 1 mg 315
Antagonists 4558 emPA Highly potent and selective oX2 antagonist; brain penetrant 10 mg
50 mg
209
879
4317 JnJ 10397049 Selective oX2 receptor antagonist 10 mg
50 mg
195
819
1960 SB 334867 Selective non-peptide oX1 antagonist 1 mg
10 mg
50 mg
95
195
819
1963 SB 408124 Selective non-peptide oX1 antagonist 10 mg 239
3818 TCS 1102 Potent antagonist of oX1 and oX2 10 mg
50 mg
155
655
3371 TCS oX2 29 Potent and selective oX2 antagonist 10 mg
50 mg
195
819
VIP and PACAP Receptors
Agonists 2711 Bay 55-9837 Potent and selective VPAC2 agonist 1 mg 325
1183 PACAP 1-27 Potent stimulator of adenylyl cyclase 100 µg 139
1186 PACAP 1-38 Potent stimulator of adenylyl cyclase 100 µg 179
2080 PHm 27 (human) endogenous peptide product of human prepro-ViP 1 mg 205
1386 [Ala11,22,28]ViP Potent, highly selective VPAC1 agonist 1 mg 399
1911 ViP (human, rat, mouse, rabbit, canine, porcine)
involved in neurotransmission, smooth muscle relaxation 1 mg 169
Antagonists 1172 [Ac-Tyr1,d-Phe2]GrF 1-29, amide (human)
ViP antagonist 500 µg 185
3236 PACAP 6-38 Potent PAC1 receptor antagonist 100 µg 145
3054 [d-p-Cl-Phe6,Leu17]-ViP Selective ViP receptor antagonist 1 mg 259
1905 ViP (6-28) (human, rat, porcine, bovine)
ViP antagonist 1 mg 255
PePTide Hormone reCePTorS
www.tocris.com | 15
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.
His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2
Exendin-4 (1933)Potent GLP-1 receptor agonist
His-Ala-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-
Glu-Phe-Ile-Ala-Trp-Leu-Val-Lys-Gly-Arg-NH2
Glucagon-like peptide 1 (7-36) amide (human, rat) (2082)Potent insulinotropic peptide
Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-
Pro-Pro-Pro-Ser-NH2
Exendin-3 (9-39) amide (2081)Potent GLP-1 receptor antagonist
O
OO
O
OHH
H
OMe
OMe
MeO
Picropodophyllotoxin (2956)Selective IGF1R inhibitor
Key Products for Glucagon and Related Receptors
Category Cat. No. Product Name Description Unit Size USD
Amylin Receptor
Agonists 3418 Amylin endogenous peptide agonist for amylin, calcitonin, CGrP and adrenomedullin receptors
500 µg 235
Antagonists 3419 AC 187 Potent and selective amylin receptor antagonist 500 µg 295
Gastric Inhibitory Polypeptide (GIP) Receptor
Agonists 2257 GiP (1-39) Highly potent insulinotropic peptide 1 mg 339
2084 GiP (human) Potent insulinotropic gut hormone 1 mg 389
Glucagon Receptor
Antagonists 2216 des-His1-[Glu9]-Glucagon (1-29) amide
Glucagon receptor antagonist 1 mg 285
2311 L-168,049 Potent, orally active human glucagon receptor antagonist 10 mg
50 mg
155
655
Glucagon-like Peptide 1 (GLP-1) Receptor
Agonists 1933 exendin-4 Potent GLP-1 receptor agonist 1 mg 339
1851 Glucagon-like peptide 1 (1-37) (human, rat)
endogenous pancreatic peptide 1 mg 389
2082 Glucagon-like peptide 1 (7-36) amide (human, rat)
Potent insulinotropic peptide 1 mg 389
Antagonists 2081 exendin-3 (9-39) amide Potent GLP-1 receptor antagonist 1 mg 389
3266 GLP-1 (9-36) amide metabolite of GLP-1-(7-36) (Cat. no. 2082) 1 mg 295
Other 2094 oxyntomodulin endogenous gut peptide; modulates feeding and metabolism 1 mg 315
Glucagon-like Peptide 2 (GLP-2) Receptor
Other 2258 GLP-2 (human) endogenous hormone; displays intestinotropic activity 1 mg 265
2259 GLP-2 (rat) endogenous hormone; displays intestinotropic activity 1 mg 265
Insulin Receptor
Activators 1819 demethylasterriquinone B1 Selective insulin rTK activator 5 mg 219
Agonists 3435 insulin (human) recombinant, expressed in yeast
endogenous insulin receptor peptide agonist 10 mg 75
Insulin-like Growth Factor 1 Receptor (IGF1R)
Inhibitors 2956 Picropodophyllotoxin Selective iGF1r inhibitor 10 mg 195
2768 PQ 401 iGF1r inhibitor 10 mg
50 mg
145
609
Tocris Product Listing Series
16 |
other Peptide HormonesNumerous 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
N
SO O
HN
O
NH2
SO
O
L-368,899 (2641)Potent, non-peptide oxytocin receptor antagonist
NNHN
N
OO
HO
HO NH
NN
WAY 267464 (3933)Potent, non-peptide oxytocin receptor agonist
Key Products for Oxytocin Receptors
Category Cat. No. Product Name Description Unit Size USD
Calcitonin Receptor
Agonists 1161 CGrP (rat) Potent vasodilator 100 µg 135
2550 SUn-B 8155 non-peptide calcitonin receptor agonist 10 mg
50 mg
155
655
Neuropeptide FF/AF (NPFF) Receptors
Agonists 3137 neuropeptide FF endogenous nPFF1 and nPFF2 agonist 1 mg 135
4683 rFrP 3 (human) nPFF1 agonist; GniH homolog 1 mg 135
Antagonists 2707 BiBP 3226 mixed nPFF and nPY Y1 receptor antagonist 1 mg
10 mg
129
275
3672 rF 9 Selective nPFF1 and nPFF2 antagonist 1 mg 105
Ligands 1486 Gr 231118 nPFF receptor ligand. Also nPY Y1 antagonist/nPY Y4 agonist 500 µg 339
Oxytocin Receptor
Agonists 4852 Carbetocin oxytocin analog 10 mg 149
1910 oxytocin involved in uterine contraction and lactation 1 mg 75
3933 WAY 267464 Potent, non-peptide oxytocin receptor agonist 10 mg 239
Antagonists 2641 L-368,899 Potent, non-peptide oxytocin receptor antagonist 1 mg
10 mg
135
289
2410 L-371,257 Potent and selective oxytocin receptor antagonist 10 mg 219
Parathyroid Hormone Receptors
Agonists 3011 Parathyroid hormone (1-34) (human) Parathyroid hormone receptor agonist 1 mg 305
PePTide Hormone reCePTorS
www.tocris.com | 17
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.
Category Cat. No. Product Name Description Unit Size USD
Angiotensin-converting Enzyme (ACE)
Inhibitors 2578 Benazepril ACe inhibitor 50 mg 129
4455 Captopril ACe inhibitor; also inhibits LTA4 hydrolase 50 mg 59
2691 moexipril ACe inhibitor 10 mg
50 mg
139
585
4302 Perindopril ACe inhibitor 50 mg 115
2931 Spinorphin enkephalin-degrading and ACe inhibitor 1 mg 129
Substrates 1563 Angiotensin i (human, mouse, rat) endogenous peptide substrate of ACe 1 mg 75
1764 Hemopressin (rat) Bioactive substrate for endopeptidase 24.15, neurolysin and ACe 1 mg 325
Chymase
Substrates 3841 reTF-4nA Selective chymase substrate 1 mg 155
Dipeptidyl Peptidase IV (DPP-IV)
Inhibitors 2783 dPPi 1c dipeptidyl peptidase iV inhibitor 1 mg
10 mg
105
219
2790 K 579 dipeptidyl peptidase iV inhibitor 10 mg
50 mg
219
925
3506 nVP dPP 728 Potent, orally active dipeptidyl peptidase iV inhibitor 10 mg
50 mg
195
819
4145 PK 44 Potent and selective dipeptidyl peptidase iV inhibitor 10 mg 285
Endothelin-converting Enzyme (ECE)
Inhibitors 2512 CGS 35066 endothelin-converting enzyme inhibitor 10 mg 249
Neurotensin-degrading Enzymes
Inhibitors 2575 JmV 390-1 inhibits multiple neurotensin and neuromedin n degrading enzymes
1 mg 115
Tripeptidyl Peptidase II
Inhibitors 1323 Butabindide Potent, competitive inhibitor of CCK-inactivating serine protease (tripeptidyl peptidase ii)
10 mg
50 mg
185
779
Prices are correct for 2016. For a full product listing please visit www.tocris.com
Tocris Product Listing Series
18 |
related literature from Tocris that you may be interested in:
Nuclear Receptors Product Listingover 150 products for nuclear receptors
our new product listing contains products for key nuclear receptors including:
• Androgen receptors• estrogen receptors• retinoic Acid receptors• retinoid X receptors• Vitamin d receptors
Seven-Transmembrane Receptor SignalingT. Kenakin, GlaxoSmithKline research and development r. Lefkowitz and J. Violin, duke University medical Center michael Bouvier and Geneviève oligny-Longpré, Université de montréal
Seven-transmembrane (7-Tm)-receptors are now recognized as complex processors of information that can bind to molecules and cytosolic interactants on the cell membrane. The 7-Tm poster highlights the multiple behaviours of 7-Tms including G-protein-dependent and -independent signaling as well as the concept of collateral efficacy.
Cardiovascular Research Product Guideover 250 products for Cardiovascular research
our new guide contains products with supporting information and figures to illustrate the relevance of each target within the areas of:
• Hypertension• Thrombosis and Hemostasis• Atherosclerosis• myocardial infarction and ischemia/reperfusion injury• Arrhythmias• Heart Failure
Gut Hormones and the Regulation of AppetiteV. Taylor, P. Jethwa, C. Small and S. Bloom, imperial College London
The gastrointestinal tract is the largest endocrine gland in the human body, secreting hormones that affect digestion, appetite and energy expenditure. neuropeptide modulators and gut hormones that influence appetite are reviewed in this poster.
Peptides Involved in Appetite ModulationS. Tucci, L. Koblis and T. Kirkham, University of Liverpool
A synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis. This review outlines the putative roles of most of the known peptides, and lists compounds available from Tocris.
To download or request copies, please visit www.tocris.com/requestliterature
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