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Home , Antalarmin, Apelin, Apelin receptor, Atosiban, Binaltorphimine, Bradykinin

Receptors Product Listing | Edition 2

Oriental Fire-bellied Toad Bombina orientalis A source of Products for: • Regulation • Cardiovascular Regulation • Feeding and Regulation • Regulation • Other Peptide • Processing Tocris Product Listing Series Contents This 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 , , feeding, appetite and blood glucose levels. A product listing of nuclear compounds is also available from www.tocris.com.

Anterior Pituitary Regulation...... 4 (NMU) Receptors...... 13

Corticotropin-releasing Factor (CRF) Receptors...... 4 B/W (NPBW) Receptors...... 13

Gonadotropin-releasing Hormone (GnRH) Receptors.... 4 Receptors...... 13

Kisspeptin Receptors...... 5 (NPY) Receptors...... 13

Neurotensin (NT) Receptors...... 5 Receptors...... 14

Somatostatin (sst) Receptors...... 5 Glucose Regulation...... 15

Thyrotropin-releasing Hormone (TRH) Receptors...... 5 Receptors...... 15

Gastric Inhibitory Polypeptide (GIP) Receptors...... 15 Cardiovascular Regulation...... 6

Glucagon Receptors...... 15 (AT) Receptors...... 6

Glucagon-like Peptide 1 (GLP-1) Receptor...... 15 (APJ) Receptors...... 6 Glucagon-like Peptide 2 (GLP-2) Receptor...... 15 Receptors...... 7 and Insulin-like Receptors...... 15 and Related Receptors...... 7 Other Peptide Receptors...... 16 (ET) Receptors...... 7 Calcitonin Receptors...... 16 Receptors (NPR)...... 8 Mas-Related G -Coupled Receptors...... 16 Tachykinin (NK) Receptors...... 8 Neuropeptide FF/AF Receptors...... 16 Urotensin-II (UT) Receptors...... 9 Receptors...... 17 Receptors...... 10 Receptors...... 17 Feeding and Appetite Regulation...... 10 PACAP Receptors...... 18 Bombesin (BB) Receptors...... 10 Receptors...... 18 CART...... 10 VIP Receptors...... 18 (CCK) Receptors...... 10 Peptide Hormone Processing...... 19 (GAL) Receptors...... 11 ...... 19

Ghrelin Receptors...... 11 Angiotensin-converting (ACE)...... 19

GPR103 (QRFP Receptor)...... 11 Chymase...... 19

GPR171...... 12 IV (DPP IV)...... 19

GPR83...... 12 Endothelin-converting (ECE)...... 19

Leptin Receptors...... 12 Insulin-degrading Enzyme (ICE)...... 19

Melanin-concentrating Hormone (MCH) Receptors..... 12 -degrading Enzymes...... 19

Melanocortin (MC) Receptors...... 12 ...... 19

Motilin Receptors...... 13 II...... 19

2 | PEPTIDE HORMONE RECEPTORS Introduction Most hormones are endogenous mediators secreted by endocrine glands as part of . There are three types of hormone: peptide, steroid and amine hormones. Peptide hormones are generally hydrophilic molecules that do not freely diffuse across 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 (that is, they are GPCRs). One notable exception is the , 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 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 on a variety of different disorders. Research into endocrine disorders is facilitated by the use of and antagonists active at peptide hormone receptors.

Figure 1 | Peptide receptors involved in physiological processes

Liver and Glucose Regulation Anterior Pituitary Regulation Amylin Receptor CRF Receptors GIP Receptor GnRH Receptors Receptor Glucagon-like Peptide 1 Receptor Neurotensin Receptors Glucagon-like Peptide 2 Receptor Receptors Insulin and Insulin-like Receptors TRH Receptors

Stomach and Gut Appetite Feeding Regulation Bombesin Receptors CART CCK Receptors Galanin Receptors & Ghrelin-related Receptors GPR103 (QRFP Receptor) GPR171 , Arteries and Kidneys GPR83 Cardiovascular Regulation Receptors Angiotensin Receptors MCH Receptors Apelin Receptors Receptors Bradykinin Receptors Receptors CGRP Receptor Neuromedin U Receptors Endothelin Receptors Neuropeptide B/W Receptors Natriuretic Peptide Receptors Tachykinin Receptors Neuropeptide Y Receptors Urotensin-II Receptor Orexin Receptors Vasopressin Receptors

Tocris has a broad range of products for peptide hormone receptors, including small molecules and . 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.

www.tocris.com | 3 Tocris Product Listing Series Anterior Pituitary Regulation The anterior pituitary gland is regulated by hypothalamic hormones such as somatostatin, -releasing hormone and thyrotropin-releasing hormone. Stimulation by the influences the release of hormones from the anterior pituitary, including , and adrenocorticotropic hormone (ACTH).

Category Cat. No. Product Name Description Unit Size Corticotropin-releasing Factor Receptors

Agonists 6450 Cortagine Potent and selective CRF1 100 µg 1151 CRF (, rat) Stimulates ACTH release 200 µg 1609 CRF agonist 500 µg

1608 Stressin I CRF1 agonist 500 µg 1604 (human) Endogenous CRF agonist 1 mg 1605 Urocortin (rat) Endogenous CRF agonist 1 mg

Antagonists 2778 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 Potent and selective CRF1 antagonist; 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

High Affinity CRF1 Potent and Selctive CRF1 Antagonist R 121919 Cat. No. 6530 CP 376395 Cat. No. 3212

N NH N

N N O

N N

N

R 121919 is a high affinity corticotropin release factor receptor 1 CP 376395 is an orally active, potent and selective corticotropin (CRF1) antagonist (Ki = 3.5 nM). It reduces -induced release factor receptor 1 (CRF1) antagonist (Ki values are 12 elevations of plasma ACTH in rats. R 121919 also dispays and >10000 nM for CRF1 and CRF2, respectively). It attenuates anxiolytic and effects in vivo, and it is orally CRF-induced activationCP of 376395 the HPA C axisat. N ino. vivo3212. bioavailable R 121919 Cat. No. 6530

4 | PEPTIDE HORMONE RECEPTORS

Category Cat. No. Product Name Description Unit Size 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 agonist 1 mg 1909 Neurotensin Endogenous and endocrine modulator 1 mg

5087 TC NTR1 17 Selective NTS1 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 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 Synthetic thyrotropin-releasing hormone analog 1 mg 10 mg

Key Products for Anterior Pituitary Regulation H N

N O OMe O F HN O H H O N N N N NH2 N D-Phe-His-Leu-Leu-Arg-Lys-Met-Ile-Glu-Ile- H H N O Glu-Lys-Gln-Glu-Lys-Glu-Lys-Gln-Gln-Ala- NH2 NH O Ala-Asn-Asn-Arg-Leu-Leu-Leu-Asp-Thr-Ile-NH2 F O

L-803,087 (1979) Antisauvagine-30 (2071) Taltirelin (2672)

Potent and selective sst4 agonist Potent, selective and competitive CRF2 antagonist Synthetic TRH analog

www.tocris.com | 5 Tocris Product Listing Series Cardiovascular Regulation Blood 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 prompts the release of vasopressin, increasing blood pressure.

Category Cat. No. Product Name Description Unit Size 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 4553 Azilsartan Potent AT1 receptor inverse agonist; antihypertensive 10 mg Agonists 50 mg

Antagonists 4791 Candesartan AT 1 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 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 100 µg 5966 ML 233 Non-peptide apelin receptor agonist 10 mg 50 mg

Key Products for Apelin Receptors

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

ELA-14 (Human) (6293) {Pyr1}-Apelin-13 (2420) Potent apelin agonist Potent peptide apelin agonist

N Gln-Arg-Pro-Val-Asn-Leu-Thr-Met-Arg-Arg- S N Lys-Leu-Arg-Lys-His-Asn-Cys-Leu-Gln-Arg- O O Arg-Cys-Met-Pro-Leu-His-Ser-Arg-Val-Pro- Phe-Pro O O ELA-32 (Human) (6291) O2N Potent and high affinity apelin agonist ML 221 (4748) stimulates angiogenesis Apelin antagonist

6 | PEPTIDE HORMONE RECEPTORS

Category Cat. No. Product Name Description Unit Size 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 9 3005 [Des-Arg ]-Bradykinin agonist (B1 > B2) 5 mg 8 9 3229 [Phe Ψ(CH-NH)-Arg ]-Bradykinin Selective B2 agonist 1 mg 8 9 3230 Sar-[D-Phe ]-des-Arg -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 (human, porcine) agonist; potent vasoconstrictor peptide 100 µg 1164 (human) Endothelin receptor agonist 100 µg 1162 (human, rat) Endothelin receptor agonist; potent vasoconstrictor 100 µg

1196 IRL-1620 Highly selective ETB agonist 500 µg

1175 S6c Selective ETB agonist 100 µg

Key Products for Angiotensin and Endothelin Receptors

O

N Ph HC N 2 N MeO KN N HO C N O N N 2 Cl N

NMe N N 2 O OH HO Me PD 123319 (1361) (5828) Losartan potassium (3798)

Potent and selective non-peptide AT2 antagonist Selective ETA antagonist Selective non-peptide AT1 antagonist

O NaO2C MeO

N O NH Me O H Cys-Ser-Cys-Ser-Ser-Leu-Met-Asp-Lys-Glu- N N N H Cys-Val-Tyr-Phe-Cys-His-Leu-Asp-lle-Ile-Trp O Me Me3C

Endothelin 1 (human, porcine) (1160) BQ 788 (1500)

Endothelin receptor agonist; potent vasocontrictor peptide Selective ETB antagonist

www.tocris.com | 7 Tocris Product Listing Series

Category Cat. No. Product Name Description Unit Size

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 High affinity endothelin receptor antagonist; orally bioavailable 10 mg 50 mg

1500 BQ 788 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-250 0 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) Endogenous peptide regulating blood pressure 1 mg (human, porcine) 1912 Atrial natriuretic factor (1-28) (rat) Endogenous peptide regulating blood pressure 1 mg 3522 Brain natriuretic peptide (1-32) Endogenous peptide agonist at ANP receptor A (NPR1) 1 mg (human) 3520 C-type natriuretic peptide (1-22) Endogenous peptide agonist at NPR2 500 µg (human, rat, swine) 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 8 1640 [bAla ]-(4-10) NK2 agonist 1 mg 5 9 10 3228 [Lys ,MeLeu ,Nle ]-NKA(4-10) Selective NK2 agonist 1 mg 1582 (human, porcine) Endogenous tachykinin peptide 1 mg

1068 Senktide NK3 agonist 500 µg 1156 Sensory neuropeptide; inflammatory mediator 5 mg 9 11 1178 [Sar ,Met(O2) ]-Substance P Potent and selective NK1 agonist 1 mg Antagonists 1954 Antagonist G Broad spectrum antagonist 1 mg

6486 Potent long-acting hNK1 antagonist 50 mg

3649 CP 122721 High affinity NK1 receptor antagonist 5 mg 25 mg

Key Products for Other Cardiovascular Peptide Receptors

Gly-Leu-Ser-Lys-Gly-Cys-Phe-Gly-Leu-Lys- Leu-Asp-Arg-Ile-Gly-Ser-Met-Ser-Gly-Leu- O Gly-Cys HN O N C-type natriuretic peptide (1-22) (human, rat, swine) (3520) O Endogenous peptide agonist at NPR2 O S O NH2 N O N N O O Ac-Lys-Arg-Pro-Pro-Gly-Phe-Ser-DβNal-Ile Cl Br HN HN N R 715 (3407) O N N N Potent and selective B1 antagonist HO O O OH

Br Arg-Cys-Cha-Gly-Gly-Arg-Ile-Asp-Arg-Ile- BIBN 4096 (4561) SSR 149415 (6195) Potent and selective CGRP antagonist D-Tic-Arg-Cys-NH2 Potent and selective vasopressin V1B antagonist A 71915 (6715) Highly potent and competitive NPRA antagonist

8 | PEPTIDE HORMONE RECEPTORS Cardiovascular Regulation – continued

Category Cat. No. Product Name Description Unit Size

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 analog and broad spectrum neuropeptide receptor 1 mg Substance P antagonist/inverse agonist; anticancer in vitro 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 V1B and V2 agonist; synthetic vasopressin analog 1 mg 2935 [Arg8]-Vasopressin Endogenous vasopressin agonist; antidiuretic hormone 1 mg 4 8 3127 d[Leu ,Lys ]-VP Selective V1B agonist 1 mg

Antagonists 6830 Very high affinity vasopressin 1AV 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 Potent and selective V2 antagonist; renoprotective and orally active 10 mg 50 mg 1 2 8 3377 (d(CH2)5 ,Tyr(Me) ,Arg )- Selective V1A antagonist 1 mg Vasopressin

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

www.tocris.com | 9 Tocris Product Listing Series Feeding and Appetite Regulation Feeding 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 , which stimulate feeding. Gastrointestinal hormones such as cholecystokinin influence following food intake.

Category Cat. No. Product Name Description Unit Size Bombesin Receptors Agonists 5600 BA 1 Potent bombesin agonist 1 mg 2716 BIM 187 Bombesin agonist 1 mg 1149 Bombesin Bombesin agonist; involved in function 1 mg

1789 GRP (human) Endogenous BB2 agonist 1 mg

1788 GRP (porcine) Endogenous BB2 agonist 1 mg

1908 (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 I (human) Selective CCK2 agonist 1 mg

Antagonists 2607 CI 988 Potent and selective CCK2 antagonist 10 mg 50 mg

2304 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 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

Key Products for CCK, Galanin and Ghrelin Receptors

nOctanoyl Gly-Ser-Ser-Phe-Leu-Ser-Pro-Glu-His-Gln- Glp-Gln-Asp-Tyr(SO 3 H)-Thr-Gly-Trp-Met- Asp-Phe-NH O Lys-Ala-Gln-Gln-Arg-Lys-Glu-Ser-Lys-Lys- 2 N Pro-Pro-Ala-Lys-Leu-Gln-Pro-Arg H Caerulein (6264) N N CCK agonist N H Ghrelin (rat) (1465) O Endogenous ghrelin receptor agonist

F N Gly-Trp-Thr-Leu-Asn-Ser-Ala-Gly-Tyr-Leu- N N Devazepide (2304) Leu-Gly-Pro-His-Ala-Ile-Asp-Asn-His-Arg- O Selective, orally active CCK1 antagonist Ser-Phe-Ser-Asp-Lys-His-Gly-Leu-Thr-NH2 O

YIL 781 (3959) Galanin (1-29) (rat, mouse) (2696) Ghrelin receptor (GHS-R1a) antagonist Non-selective agonist

10 | PEPTIDE HORMONE RECEPTORS

Category Cat. No. Product Name Description Unit Size 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 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 5830 K-(d-1-Nal)-FwLL-NH2 High affinity and potent ghrelin inverse agonist 1 mg Agonists 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 1 mg but is active in vivo 2951 [Des-octanoyl]-Ghrelin (rat) Major circulating form of ghrelin; devoid of activity at GHS receptor 1 mg 5560 (human) Endogenous reported anorexigenic peptide 1 mg GPR103 Ligands 4402 26RFa Ligand of GPR103; orexigenic neuropeptide 1 mg

Potent Galanin Receptor Agonist Selective non-peptide OX1 Antagonist Spexin Cat. No. 6090 SB 334867 Cat. No. 1960

N Asn-Trp-Thr-Pro-Gln-Ala-Met-Leu-Tyr-Leu- Lys-Gly-Ala-Gln-NH2 N H HN N O Me O Spexin is a potent and 3 (GAL2/GAL3) agonist N (EC values are 45.7 and 112.2 nM, respectively. This compound 50 SB 334867 is a selective non-peptide orexin OX receptor exhibits no significant activity at GAL receptors. 1 1 antagonist (pK = 7.2 for inhibition of intracellular Ca2+ release In mice and rats withSp diet-inducedexin Cat. N ,o. 6090 spexin inhibits long b in CHO cells expressing human OX ). This compound blocks chain fatty acid uptake by adipoctyes and decreases food intake. 1 orexin A-induced grooming and feeding following systemic It also exhibits anxiolytic effects in vivo. administration inSB vivo 334867. Cat. No. 1960

www.tocris.com | 11 Tocris Product Listing Series

Category Cat. No. Product Name Description Unit Size 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 8 4272 [D-Trp ]-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

Key Products for Melanocortin and Orexin Receptors

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

Thr-Cys-Ser-Cys-Arg-Leu-Tyr-Glu-Leu-Leu-

HN His-Gly-Ala-Gly-Asn-His-Ala-Ala-Gly-Ile- Leu-Thr-Leu-NH2 OMe N MeO N HN O Orexin A (human, rat, mouse) (1455)

N N Endogenous agonist at OX1 and OX2 H O MeO N Ser-Tyr-Ser-Met-Glu-His-Phe-Arg-Trp-Gly- N Lys-Pro-Val-Gly-Lys-Lys-Arg-Arg-Pro-Val- O MeO Lys-Val-Tyr-Pro-Asn-Gly-Ala-Glu-Asp-Glu- Cl Ser-Ala-Glu-Ala-Phe-Pro-Leu-Glu-Phe THIQ (3032) ACT 335827 (4983) Potent and selective MC receptor agonist 4 ACTH (1-39) (3492) Potent and selective OX1 antagonist

Potent endogenous MC2 agonist

12 | PEPTIDE HORMONE RECEPTORS Feeding and Appetite Regulation – continued

Category Cat. No. Product Name Description Unit Size

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 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 antagonist 1 mg 4934 MA 2029 Potent and selective, competitive motilin antagonist; orally active 10 mg 50 mg Neuromedin U Receptors

Agonists 3648 (rat) Potent endogenous NMU1 and NMU2 agonist 500 µg 1917 Neuromedin U (rat) Endogenous modulator of blood pressure and flow, gut ion transport, feeding 1 mg and body temperature 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 31 34 1176 [Leu ,Pro ]-Neuropeptide Y NPY Y1 agonist 200 µg (human, rat) 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 (human) NPY Y4 agonist; involved in gastrointestinal tract function 200 µg 1-7 19-23 31 32 1365 [cPP ,NPY ,Ala ,Aib , Potent and selective NPY Y5 agonist 1 mg Gln34] - hPancreatic Polypeptide

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

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

Key Products for Neuropeptide Y Receptors H2N NH

HN

O O O NH O N N N H N NH2 H H N HN HN O O Tyr-Pro-Ser-Lys-Pro-Asp-Asn-Pro-Gly-Glu- HN HN NH N 2 Asp-Ala-Pro-Ala-Glu-Asp-Met-Ala-Arg-Tyr- N Tyr-Ser-Ala-Leu-Arg-His-Tyr-Ile-Asn-Leu- O N O O Leu-Thr-Arg-Pro-Arg-Tyr-NH2

BIBO 3304 (2412) [Leu31,Pro34]-Neuropeptide Y BIIE 0246 (1700)

Highly selective NPY Y1 (human, rat) (1176) Potent, selective non-peptide

receptor antagonist NPY Y1 receptor agonist NPY Y2 receptor antagonist

www.tocris.com | 13 Tocris Product Listing Series Feeding and Appetite Regulation – continued

Category Cat. No. Product Name Description Unit Size

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 11 15 Agonists 2142 [Ala ,D-Leu ]-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 antagonist 10 mg 50 mg

3371 TCS OX2 29 Potent and selective OX2 antagonist 10 mg 50 mg

14 | PEPTIDE HORMONE RECEPTORS Glucose Regulation Glucose 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 . 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 Amylin Receptors Agonists 3418 Amylin Endogenous peptide agonist for amylin, calcitonin, CGRP and 500 µg receptors 6030 Amylin (rat) Potent endogenous peptide agonist for amylin, calcitonin, CGRP and 500 µg adrenomedullin receptors 5031 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 Glucagon receptor antagonist 1 mg (1-29) 2311 L-16 8,0 49 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) Endogenous pancreatic peptide 1 mg (human, rat) 2082 Glucagon-like peptide 1 (7-36) Potent insulinotropic peptide 1 mg amide (human, rat) 6517 Potent, long-acting GLP-1 agonist 1 mg 2094 (porcine, bovine) GLP-1 receptor agonist; modulates feeding and 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 -I binding protein (IGFBP) inhibitor 10 mg 50 mg

www.tocris.com | 15 Tocris Product Listing Series Other Peptide Receptors Numerous processes are influenced by peptide hormones, including regulation (calcitonin and parathyroid hormone), uterine contraction (oxytocin) and (neuropeptide FF). Regulation of calcium homeostasis is of particular importance in .

Category Cat. No. Product Name Description Unit Size Calcitonin Receptors Agonists 6031 Calcitonin (human) Endogenous calcitonin agonist; inhibits 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 -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 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 1 mg MRGPRA agonist 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

Key Products for Oxytocin Receptors O O

N O Ala-Val-Ser-Glu-Ile-Gln-Leu-Met-His-Asn- Leu-Gly-Lys-His-Leu-Ala-Ser-Val-Glu-Arg- N N Met-Gln-Trp-Leu-Arg-Lys-Lys-Leu-Gln-Asp- Val-His-Asn-Phe N O OMe O HO Parathyroid hormone (1-34) (rat) (6301) L-371,257 (2410) Parathyroid hormone (PTH) receptor agonist Potent and selective antagonist HO O H N NH O NH S O Et2N H O OMe N Me HO O OH Me N fluorescein (6046) Cys-Tyr-Ile-Gln-Asn-Cys-Pro-Leu-Gly-NH2 Fluorescent ; fluorescent-derivative of naloxone (Cat. No. 0599) SNC 80 (0764) Oxytocin (1910) Highly selective non-peptide δ agonist Involved in uterine contraction and lactation

16 | PEPTIDE HORMONE RECEPTORS

Category Cat. No. Product Name Description Unit Size Opioid Receptors Agonists 4335 AR-M 1000390 Low-internalizing δ agonist 10 mg 50 mg 2808 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 A Endogenous κ agonist 1 mg 3196 Endogenous κ agonist 1 mg 1055 -1 Potent and selective μ agonist 5 mg 5158 opioid 50 mg 1780 NNC 63-0532 Potent non-peptide NOP agonist; brain penetrant 10 mg 50 mg 0910 Endogenous NOP agonist 1 mg

0921 SB 205607 Selective, high affinity non-peptideδ 1 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 10 mg (Cat. No. 0495) 50 mg Antagonists 0347 nor- 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 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 100 µg (Cat. No. 0599) 0599 Naloxone Non-selective opioid antagonist 100 mg 0677 Non-selective opioid antagonist 100 mg 0892 Standard δ2 selective antagonist 10 mg 50 mg 0740 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 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 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

www.tocris.com | 17 Tocris Product Listing Series

Other Peptide Hormones – continued

Category Cat. No. Product Name Description Unit Size PACAP Receptors Agonists 1183 PACAP 1-27 Endogenous neuropeptide; potent stimulator of 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) Parathyroid hormone (PTH) receptor agonist 1 mg (bovine) 3011 Parathyroid hormone (1-34) Parathyroid hormone (PTH) receptor agonist 1 mg (human) 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, Involved in and relaxation 1 mg canine, porcine) Antagonists 3054 [D-p-Cl-Phe6,Leu17]-VIP Selective VIP receptor antagonist 1 mg 1905 VIP (6-28) (human, rat, porcine, VIP receptor antagonist 1 mg bovine)

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

Category Cat. No. Product Name Description Unit Size Aminopeptidases Inhibitors 1956 Bestatin 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 ACE inhibitor; also inhibits LTA4 50 mg 4302 Perindopril Angiotensin-converting enzyme (ACE) inhibitor 50 mg 2931 -degrading and ACE inhibitor 1 mg Ligand 6006 Acein High affinity angiotensin-converting enzyme (ACE) ligand 1 mg 3791 (human, mouse) Bioactive substrate for 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; activein vivo 10 mg 50 mg Endothelin-converting Enzyme Inhibitors 2512 CGS 35066 Endothelin-converting enzyme (ECE) inhibitor 10 mg 6333 disodium salt Neutral endopeptidase and endothelin converting 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 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 inhibitor 10 mg 50 mg

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