Peptide Hormone Receptors - Tocris Bioscience · 2017. 5. 25. · Gonadotropin-releasing Hormone...

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

Product Listing | Edition 1

Tocris Product Listing Series

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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.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

Corticotropin-releasing Factor (CRF) Receptors

Agonists 1151 CrF (human, rat) Stimulates ACTH release 200 µg1608 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 mg50 mg

2071 Antisauvagine-30 Potent, selective and competitive CrF2 antagonist 1 mg

1606 Astressin Potent CrF receptor 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 receptor 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

3294 Sn 003 Potent and selective CrF1 antagonist 10 mg

Other 1607 CrF (6-33) CrF binding protein inhibitor 1 mgGonadotropin-releasing Hormone (GnRH) Receptors

Agonists 3592 Goserelin acetate GnrH receptor agonist 10 mg2873 Leuprolide GnrH receptor agonist 1 mg

2544 nafarelin GnrH receptor agonist 1 mg

Antagonists 2730 AG 045572 Selective GnrH receptor antagonist 1 mg10 mg

3536 Cetrorelix acetate Potent GnrH antagonist 1 mg

2519 T 98475 GnrH receptor antagonist 1 mg


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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


Kisspeptin Receptor

Agonists 2570 Kisspeptin 10 (human) endogenous ligand for KiSS1 receptor 1 mg4243 Kisspeptin 10 (rat) endogenous ligand for KiSS1 receptor 1 mg

Antagonists 3881 Kisspeptin 234 KiSS1/GPr54 antagonist; kisspeptin 10 (Cat. no. 2570) analog 1 mgNeurotensin (NT) Receptors

Agonists 1998 JmV 449 Potent neurotensin receptor agonist 1 mg1909 neurotensin endogenous neurotransmitter and endocrine modulator 1 mg

Antagonists 2309 Sr 142948 Highly potent neurotensin receptor antagonist 1 mg10 mg

3721 Sr 48692 Selective non-peptide nTS1 antagonist 10 mg

50 mg

Somatostatin (sst) Receptors

Agonists 2842 Bim 23052 sst5 agonist 1 mg2454 CH 275 Potent and selective sst1 receptor agonist 1 mg

2444 (1R,1ʹS,3ʹR/1R,1ʹR,3ʹS)-L-054,264 Potent and selective sst2 agonist 1 mg10 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 endogenous sst agonist; influences growth hormone release 1 mg

1165 Somatostatin 1-28 sst receptor agonist 500 µg

4639 TT 232 sst1/sst4 receptor agonist 1 mg

Antagonists 3493 Cyclosomatostatin non-selective sst receptor antagonist 1 mg1843 CYn 154806 Selective sst2 antagonist 1 mg

Ligands 1844 Bim 23056 Somatostatin receptor ligand 1 mgOther 3374 Cortistatin 14 endogenous neuropeptide; binds sst1 - sst5 and GHS-r1a 1 mgThyrotropin-releasing Hormone (TRH) Receptors

Agonists 2672 Taltirelin Synthetic thyrotropin-releasing hormone analog 1 mg10 mg


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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


Angiotensin (AT) Receptors

Agonists 1562 Angiotensin (1-7) Vasorelaxant peptide 1 mg1563 Angiotensin i (human, mouse, rat) endogenous precursor to angiotensin ii (Cat. no. 1158) 1 mg

1158 Angiotensin ii Potent vasoconstrictor peptide 5 mg

Antagonists 4553 Azilsartan Potent AT1 receptor inverse agonist; antihypertensive 10 mg50 mg

4792 Candesartan cilexetil Prodrug of candesartan (Cat. no. 4791), an AT1 receptor antagonist

10 mg

50 mg

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

50 mg

4696 eprosartan Potent and selective AT1 receptor antagonist 10 mg

50 mg

3798 Losartan Selective, non-peptide AT1 antagonist 50 mg

4616 olmesartan Potent AT1 antagonist 50 mg

1361 Pd 123319 Potent, 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


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Blood Pressure regulation – continued


Apelin (APJ) Receptors

Agonists 2420 [Pyr1]-Apelin-13 Potent peptide agonist for APJ receptor 1 mg3007 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

Antagonists 4748 mL 221 APJ receptor antagonist 10 mg50 mg

Bradykinin Receptors

Agonists 3004 Bradykinin endogenous agonist at bradykinin receptors (B2 > B1) 5 mg3005 [des-Arg9]-Bradykinin Bradykinin receptor agonist (B1 > B2) 5 mg

3229 [Phe8Ψ(CH-nH)Arg9]-Bradykinin Selective B2 agonist 1 mg3227 Lys-Bradykinin Potent bradykinin receptor agonist (B2 > B1) 1 mg

3225 Lys-[des-Arg9]Bradykinin Selective B1 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 µg3978 men 11270 Selective B2 antagonist; analog of Hoe 140 (Cat. no. 3014) 500 µg

1697 noscapine Bradykinin antagonist. Also tubulin inhibitor 100 mg

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 mgCalcitonin Gene-related Peptide (CGRP) Receptor

Agonists 3012 α-CGrP (human) CGrP receptor agonist 1 mgAntagonists 4561 BiBn 4096 Potent and selective CGrP receptor antagonist 10 mg

1181 CGrP 8-37 (human) CGrP1 receptor antagonist 500 µg

1169 CGrP 8-37 (rat) CGrP1 receptor antagonist 500 µg

4314 SB 268262 Selective non-peptide CGrP1 antagonist 10 mg

50 mg

Endothelin (ET) Receptors

Agonists 1189 BQ-3020 Selective eTB agonist 500 µg1160 endothelin 1 (human, porcine) Potent vasoconstrictor peptide 100 µg

1164 endothelin 2 (human) eTA/eTB agonist 100 µg

1162 endothelin 3 (human, rat) Potent vasoconstrictor 100 µg

1175 Sarafotoxin S6c Selective eTB agonist 100 µg

Antagonists 1441 BmS 182874 Highly selective, orally active non-peptide eTA antagonist 10 mg50 mg

1188 BQ-123 Selective eTA antagonist 500 µg

1500 BQ 788 Selective eTB antagonist 1 mg

1210 Fr 139317 Highly potent, selective eTA antagonist 10 mg

50 mg

1838 irL-2500 Potent eTB antagonist 10 mg

Natriuretic Peptide Receptors (NPR)

Agonists 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


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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


Tachykinin (NK) Receptors

Agonists 1668 Gr 64349 Potent, selective nK2 agonist 1 mg1669 Gr 73632 Potent, selective nK1 agonist 1 mg

1535 Hemokinin 1 (mouse) endogenous, high affinity, selective nK1 agonist 1 mg

1640 [bAla8]-neurokinin A(4-10) nK2 agonist 1 mg

1152 neurokinin A (porcine) endogenous tachykinin peptide 1 mg

1582 neurokinin B (human, porcine) endogenous tachykinin peptide 1 mg

3228 [Lys5,meLeu9,nle10]-nKA(4-10) Selective nK2 agonist 1 mg

1068 Senktide Tachykinin nK3 agonist 500 µg

1178 [Sar9,met(o2)11]-Substance P Potent, selective nK1 agonist 1 mg

1156 Substance P Sensory neuropeptide, inflammatory mediator 5 mg

Antagonists 1954 Antagonist G Broad spectrum neuropeptide receptor antagonist 1 mg2893 CP 96345 Potent and selective nK1 antagonist 10 mg

50 mg

2400 FK 888 High affinity nK1 receptor antagonist 10 mg

1274 Gr 159897 non-peptide, potent nK2 antagonist 10 mg

50 mg

1667 Gr 94800 Potent, selective nK2 antagonist 1 mg

0868 L-732,138 Potent, selective nK1 antagonist 10 mg

50 mg

1145 L-733,060 Potent nK1 antagonist 10 mg

50 mg

4013 L 760735 High affinity nK1 receptor antagonist 10 mg

50 mg

1635 rP 67580 Potent and selective nK1 antagonist 10 mg

50 mg

1376 SB 218795 Potent, selective non-peptide nK3 antagonist 10 mg

50 mg

1393 SB 222200 Potent, selective non-peptide nK3 antagonist. Brain penetrant 10 mg

50 mg

4012 Sr 140333 Potent nK1 receptor 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

1 mg


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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


Urotensin-II (UT) Receptor

Agonists 1642 Urotensin-ii (human) endogenous vasoactive agonist for the urotensin-ii receptor 1 mgAntagonists 4670 SB 611812 Urotensin-ii receptor antagonist; attenuates cardiac dysfunction 10 mg

50 mg

3571 SB 657510 Selective urotensin-ii receptor antagonist 10 mg

50 mg

2529 UFP 803 Urotensin-ii receptor antagonist 1 mg

3162 [orn5]-UrP Urotensin-ii receptor antagonist 1 mg

Vasopressin Receptors

Agonists 3396 desmopressin Synthetic vasopressin analog; V1B and V2 agonist 1 mg2935 [Arg8]-Vasopressin Antidiuretic hormone 1 mg

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

Antagonists 3924 oPC 21268 orally active vasopressin V1 antagonist 10 mg50 mg

2310 Sr 49059 Selective, orally active vasopressin V1A receptor antagonist 10 mg

3377 (d(CH2)51,Tyr(me)2,Arg8)-Vasopressin

Selective vasopressin V1A antagonist 1 mg


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


Bombesin (BB) Receptors

Agonists 2716 Bim 187 Bombesin/GrP receptor agonist 1 mg1149 Bombesin Bombesin receptor agonist; involved in gastrointestinal tract

function1 mg

1789 GrP (human) endogenous GrP receptor agonist 1 mg

1788 GrP (porcine) endogenous GrP receptor agonist 1 mg

1908 neuromedin B (porcine) mammalian bombesin-like peptide 1 mg

Antagonists 2717 Bim 189 Bombesin receptor antagonist 1 mg3237 Bim 23042 Selective BB1 receptor antagonist 1 mg

2602 Pd 176252 BB2 and BB1 receptor antagonist 10 mg

CART

Other 3339 CArT (62-76) (rat, human) neuromodulating neuropeptide fragment; inhibits food intake in vivo

1 mg

3338 CArT (55-102) (human) neuromodulatory neuropeptide fragment; satiety factor 100 µg

3337 CArT (55-102) (rat) neuromodulatory neuropeptide fragment; satiety factor 100 µg

Cholecystokinin (CCK) Receptors

Agonists 2411 A-71623 Potent and selective CCK1 agonist. Suppresses feeding 1 mg1150 CCK octapeptide, non-sulfated non-sulfated form of CCK octapeptide (Cat. no. 1166) 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 mg50 mg

2304 devazepide Selective, orally active CCK1 receptor antagonist 10 mg

50 mg

2767 L-365,260 Selective CCK2 antagonist 10 mg

50 mg

1524 LY 288513 Selective CCK2 antagonist 10 mg

50 mg


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


Antagonists 2608 Pd 135158 Potent and selective CCK2 antagonist 10 mg50 mg

1478 Proglumide 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, selective non-peptide CCK2 antagonist 10 mg

50 mg

Galanin (GAL) Receptors

Agonists 2699 Ar-m 1896 GAL2 agonist 1 mg2696 Galanin (1-29) (rat, mouse) non-selective galanin receptor agonist 1 mg

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

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

2085 Galnon non-selective galanin receptor agonist 10 mg

3629 m 1145 Potent and selective GAL2 agonist 500 µg

2697 m617 Selective GAL1 agonist 1 mg

Antagonists 3425 m40 Potent, non-selective galanin receptor antagonist 1 mg2698 m871 Selective GAL2 antagonist 1 mg

Ghrelin & Ghrelin-related Receptors

Agonists 1463 Ghrelin (human) endogenous ghrelin receptor agonist 1 mg1465 Ghrelin (rat) endogenous ghrelin receptor agonist 1 mg

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

2308 Tabimorelin Potent, orally active ghrelin receptor agonist 10 mg

Antagonists 3033 Cortistatin-8 Ghrelin receptor antagonist 1 mg1922 [d-Lys3]-GHrP-6 Ghrelin receptor antagonist 5 mg

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

3959 YiL 781 Ghrelin receptor antagonist 10 mg

50 mg

Other 3374 Cortistatin 14 endogenous neuropeptide; binds ghrelin receptor and sst1 - sst5 1 mg2260 [des-octanoyl]-Ghrelin (human) major circulating form of ghrelin; devoid of activity at ghrelin

receptor but is active in vivo1 mg

2951 [des-octanoyl]-Ghrelin (rat) major circulating form of ghrelin; devoid of activity at ghrelin receptor

1 mg

2445 obestatin (rat) endogenous anorexigenic peptide 1mg


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


GPR103 (QRFP Receptor)

Ligands 4402 26rFa Ligand of GPr103; orexigenic neuropeptide 1 mgLeptin Receptors

Other 2985 LeP (116-130) (mouse) Synthetic leptin peptide fragment 1 mgMelanin-concentrating Hormone (MCH) Receptors

Agonists 3434 [Ala17]-mCH Potent, mCH receptor agonist 1 mg3806 mCH (human, mouse, rat) Potent endogenous mCH agonist 100 µg

Antagonists 3359 ATC 0065 Potent and selective mCH1 antagonist 10 mg50 mg

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 (MC) Receptors

Agonists 3492 ACTH (1-39) Potent endogenous mC2 agonist 1 mg4053 BmS 470539 Potent, selective mC1 receptor agonist 10 mg

50 mg

2566 melanotan ii High affinity melanocortin receptor agonist 1 mg

2584 α-mSH endogenous melanocortin receptor agonist 1 mg

3013 [nle4,d-Phe7]-α-mSH melanocortin receptor agonist 1 mg

4272 [d-Trp8]-γ-mSH Selective mC3 receptor agonist 1 mg

3032 THiQ Potent and selective mC4 receptor agonist 1 mg

Antagonists 1831 HS 014 Selective mC4 receptor antagonist 1 mg1832 HS 024 Highly potent mC4 receptor antagonist 1 mg

3438 mCL 0020 Selective mC4 receptor antagonist 1 mg

Other 3420 SHU 9119 mC3 and mC4 antagonist, mC5 partial agonist 1 mgMotilin Receptors

Other 2264 motilin (human, porcine) endogenous peptide regulator of gastrointestinal motility 1 mgNeuromedin U (NMU) Receptors

Agonists 3648 neuromedin S (rat) Potent, endogenous nmU1 and nmU2 agonist 500 µg1917 neuromedin U (rat) endogenous modulator of blood pressure and flow, gut ion

transport, feeding and body temperature1 mg

Neuropeptide B/W (NPBW) Receptors

Agonists 3009 neuropeptide W-23 (human) endogenous nPBW1 and nPBW2 receptor agonist 1mg


www.tocris.com | 13


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 NH

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


Neuropeptide S Receptor

Antagonists 4510 SHA 68 Selective neuropeptide S receptor antagonist 10 mg50 mg

Neuropeptide Y (NPY) Receptors

Agonists 2035 BWX 46 Highly selective nPY Y5 agonist 1 mg1177 neuropeptide Y 13-36 (porcine) nPY Y2 receptor agonist 500 µg

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

nPY Y1 receptor agonist 200 µg

1153 neuropeptide Y (human, rat) influences feeding and sexual behavior 200 µg

1168 [Leu31,Pro34]-neuropeptide Y (porcine)

nPY Y1 receptor agonist 200 µg

1173 neuropeptide Y (porcine) influences feeding and sexual behavior 200 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, selective nPY Y5 agonist 1 mg

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

Antagonists 2412 BiBo 3304 Highly selective nPY Y1 receptor antagonist 10 mg50 mg

2707 BiBP 3226 mixed nPY Y1 and nPFF receptor antagonist 1 mg

10 mg

1700 Biie 0246 Potent, selective non-peptide nPY Y2 receptor antagonist 1 mg

10 mg

3242 BmS 193885 Potent, competitive nPY Y1 receptor antagonist 10 mg

50 mg

2199 CGP 71683 Highly selective and potent non-peptide nPY Y5 receptor antagonist

10 mg

50 mg

4606 CYm 9484 Potent nPY Y2 receptor antagonist 10 mg

50 mg

4018 JnJ 5207787 Selective nPY Y2 receptor antagonist 10 mg

50 mg

1382 L-152,804 Potent, selective non-peptide nPY Y5 receptor antagonist 10 mg

50 mg

3562 LU AA33810 Potent nPY Y5 receptor 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 receptor antagonist 10 mg

50 mg

3898 SF 11 nPY Y2 receptor antagonist 10 mg

50 mg


14 |



Opioid Receptors

Agonists 4335 Ar-m 1000390 Low-internalizing δ opioid receptor agonist 10 mg50 mg

3790 dAdLe Prototypical δ agonist 5 mg

1171 dAmGo Selective µ agonist 1 mg

4591 deltorphin 1 Potent δ agonist 1 mg

1431 dPdPe Selective δ agonist 1 mg

3195 dynorphin A endogenous k agonist 1 mg

3196 dynorphin B endogenous k agonist 1 mg

1055 endomorphin-1 Potent and selective µ agonist 5 mg

0910 nociceptin endogenous noP agonist 1 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

Antagonists 0347 nor-Binaltorphimine Standard k-selective antagonist 10 mg50 mg

0740 naltrindole δ-selective non-peptide antagonist 10 mg

50 mg

Orexin Receptors

Agonists 1455 orexin A (human, rat, mouse) endogenous agonist at oX1 and oX2 500 µg1456 orexin B (human) endogenous agonist at oX1 and oX2 500 µg

2142 [Ala11,d-Leu15]-orexin B Potent, selective oX2 receptor agonist 1 mg

Antagonists 4558 emPA Highly potent and selective oX2 antagonist; brain penetrant 10 mg50 mg

4317 JnJ 10397049 Selective oX2 receptor 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 antagonist of oX1 and oX2 10 mg

50 mg

3371 TCS oX2 29 Potent and selective oX2 antagonist 10 mg

50 mg

VIP and PACAP Receptors

Agonists 2711 Bay 55-9837 Potent and selective VPAC2 agonist 1 mg1183 PACAP 1-27 Potent stimulator of adenylyl cyclase 100 µg

1186 PACAP 1-38 Potent stimulator of adenylyl cyclase 100 µg

2080 PHm 27 (human) endogenous peptide product of human prepro-ViP 1 mg

1386 [Ala11,22,28]ViP Potent, highly selective VPAC1 agonist 1 mg

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

involved in neurotransmission, smooth muscle relaxation 1 mg

Antagonists 1172 [Ac-Tyr1,d-Phe2]GrF 1-29, amide (human)

ViP antagonist 500 µg

3236 PACAP 6-38 Potent PAC1 receptor antagonist 100 µg

3054 [d-p-Cl-Phe6,Leu17]-ViP Selective ViP receptor antagonist 1 mg

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

ViP antagonist 1 mg


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


Amylin Receptor

Agonists 3418 Amylin endogenous peptide agonist for amylin, calcitonin, CGrP and adrenomedullin receptors

500 µg

Antagonists 3419 AC 187 Potent and selective amylin receptor antagonist 500 µgGastric Inhibitory Polypeptide (GIP) Receptor

Agonists 2257 GiP (1-39) Highly potent insulinotropic peptide 1 mg2084 GiP (human) Potent insulinotropic gut hormone 1 mg

Glucagon Receptor

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

Glucagon receptor antagonist 1 mg

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

50 mg

Glucagon-like Peptide 1 (GLP-1) Receptor

Agonists 1933 exendin-4 Potent GLP-1 receptor agonist 1 mg1851 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

Antagonists 2081 exendin-3 (9-39) amide Potent GLP-1 receptor antagonist 1 mg3266 GLP-1 (9-36) amide metabolite of GLP-1-(7-36) (Cat. no. 2082) 1 mg

Other 2094 oxyntomodulin endogenous gut peptide; modulates feeding and metabolism 1 mgGlucagon-like Peptide 2 (GLP-2) Receptor

Other 2258 GLP-2 (human) endogenous hormone; displays intestinotropic activity 1 mg2259 GLP-2 (rat) endogenous hormone; displays intestinotropic activity 1 mg

Insulin Receptor

Activators 1819 demethylasterriquinone B1 Selective insulin rTK activator 5 mgAgonists 3435 insulin (human) recombinant,

expressed in yeastendogenous insulin receptor peptide agonist 10 mg

Insulin-like Growth Factor 1 Receptor (IGF1R)

Inhibitors 2956 Picropodophyllotoxin Selective iGF1r inhibitor 10 mg2768 PQ 401 iGF1r inhibitor 10 mg

50 mg


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


Calcitonin Receptor

Agonists 1161 CGrP (rat) Potent vasodilator 100 µg2550 SUn-B 8155 non-peptide calcitonin receptor agonist 10 mg

50 mg

Neuropeptide FF/AF (NPFF) Receptors

Agonists 3137 neuropeptide FF endogenous nPFF1 and nPFF2 agonist 1 mg4683 rFrP 3 (human) nPFF1 agonist; GniH homolog 1 mg

Antagonists 2707 BiBP 3226 mixed nPFF and nPY Y1 receptor antagonist 1 mg10 mg

3672 rF 9 Selective nPFF1 and nPFF2 antagonist 1 mg

Ligands 1486 Gr 231118 nPFF receptor ligand. Also nPY Y1 antagonist/nPY Y4 agonist 500 µgOxytocin Receptor

Agonists 4852 Carbetocin oxytocin analog 10 mg1910 oxytocin involved in uterine contraction and lactation 1 mg

3933 WAY 267464 Potent, non-peptide oxytocin receptor agonist 10 mg

Antagonists 2641 L-368,899 Potent, non-peptide oxytocin receptor antagonist 1 mg10 mg

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

Parathyroid Hormone Receptors

Agonists 3011 Parathyroid hormone (1-34) (human) Parathyroid hormone receptor agonist 1 mg


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.


Angiotensin-converting Enzyme (ACE)

Inhibitors 2578 Benazepril ACe inhibitor 50 mg4455 Captopril ACe inhibitor; also inhibits LTA4 hydrolase 50 mg

2691 moexipril ACe inhibitor 10 mg

50 mg

4302 Perindopril ACe inhibitor 50 mg

2931 Spinorphin enkephalin-degrading and ACe inhibitor 1 mg

Substrates 1563 Angiotensin i (human, mouse, rat) endogenous peptide substrate of ACe 1 mg1764 Hemopressin (rat) Bioactive substrate for endopeptidase 24.15, neurolysin and ACe 1 mg

Chymase

Substrates 3841 reTF-4nA Selective chymase substrate 1 mgDipeptidyl Peptidase IV (DPP-IV)

Inhibitors 2783 dPPi 1c dipeptidyl peptidase iV inhibitor 1 mg10 mg

2790 K 579 dipeptidyl peptidase iV inhibitor 10 mg

50 mg

3506 nVP dPP 728 Potent, orally active dipeptidyl peptidase iV inhibitor 10 mg

50 mg

4145 PK 44 Potent and selective dipeptidyl peptidase iV inhibitor 10 mg

Endothelin-converting Enzyme (ECE)

Inhibitors 2512 CGS 35066 endothelin-converting enzyme inhibitor 10 mgNeurotensin-degrading Enzymes

Inhibitors 2575 JmV 390-1 inhibits multiple neurotensin and neuromedin n degrading enzymes

1 mg

Tripeptidyl Peptidase II

Inhibitors 1323 Butabindide Potent, competitive inhibitor of CCK-inactivating serine protease (tripeptidyl peptidase ii)

10 mg

50 mg


18 |

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Gut Hormones and the Regulation of AppetiteV. Taylor, P. Jethwa, C. Small and S. Bloom, imperial College London

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To download or request copies, please visit www.tocris.com/requestliterature

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