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Melanocortin Receptor MC Receptor

The (MC) receptors represent a subfamily of G-protein-coupled receptors (GPCRs) where the different subtypes are involved in a wide range of physiological functions such as pigmentation, steroid secretion, energy homeostasis, and food intake. The (MCR) family consists of five G-protein-coupled receptors (MC1R-MC5R). MC1R controls pigmentation, MC2R is a critical component of the hypothalamic-pituitary-adrenal axis, MC3R and MC4R have a vital role in energy homeostasis and MC5R is involved in exocrine function.

MCRs are activated by a variety of neuropeptides, termed , that include the adrenocorticotropic hormone (ACTH) andα, β and γ-melanocyte-stimulating hormones (MSHs). Melanocortins derive from post-translational processing of the common polypeptide precursor pro-opiomelanocortin, expressed mainly in the hypothalamus and pituitary.

www.MedChemExpress.com 1 Melanocortin Receptor , Antagonists & Inhibitors

ACTH (1-17) ACTH (1-17) (TFA) (α1-17-ACTH) Cat. No.: HY-P1545 (α1-17-ACTH TFA) Cat. No.: HY-P1545A

ACTH (1-17), an adrenocorticotropin analogue, is a ACTH (1-17) TFA, an adrenocorticotropin analogue, potent human melanocortin 1 (MC1) receptor is a potent human melanocortin 1 (MC1)

with a Ki of 0.21 nM. receptor agonist with a Ki of 0.21 nM.

Purity: >98% Purity: 99.02% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 1 mg, 5 mg, 10 mg

ACTH (11-24) Adrenocorticotropic Hormone (ACTH) (1-39), rat (Adrenocorticotropic Hormone (11-24)) Cat. No.: HY-P1558 (ACTH (1-39) (mouse, rat)) Cat. No.: HY-P1477

ACTH (11-24) is a fragment of Adrenocorticotropic Hormone (ACTH) (1-39), rat is adrenocorticotrophin, acts as an antagonist of a potent melanocortin 2 (MC2) receptor adrenocorticotropic hormone (ACTH) receptor, and agonist. induces cortisol release.

Purity: 95.40% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 1 mg, 5 mg

Adrenocorticotropic Hormone (ACTH) (1-39), rat TFA Bremelanotide Acetate (ACTH (1-39) (mouse, rat) TFA) Cat. No.: HY-P1477A (PT-141 Acetate) Cat. No.: HY-18678A

Adrenocorticotropic Hormone (ACTH) (1-39), rat Bremelanotide Acetate (PT-141 Acetate), a (TFA) is a potent melanocortin 2 (MC2) synthetic analogue of α-MSH, is an agonist receptor agonist. at melanocortin receptors including the MC3R and MC4R for the treatment of .

Purity: 99.84% Purity: 99.97% Clinical Data: No Development Reported Clinical Data: Launched Size: 500 μg, 1 mg, 5 mg Size: 10 mM × 1 mL, 10 mg, 50 mg

HS014 HS014 TFA Cat. No.: HY-P1216 Cat. No.: HY-P1216A

HS014 is a potent and selective melanocortin-4 HS014 TFA is a potent and selective

(MC4) receptor antagonist, with Kis of 3.16, 108, melanocortin-4 (MC4) receptor antagonist, with

54.4 and 694 nM for human MC4, MC1, MC3 and MC5 Kis of 3.16, 108, 54.4 and 694 nM for human MC4, receptors, respectively. HS014 modulates the MC1, MC3 and MC5 receptors respectively. HS014 TFA behavioral effects of morphine in mice. HS014 modulates the behavioral effects of morphine in increases food intake in free-feeding rats. mice. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg

HS024 HS024 TFA Cat. No.: HY-P1215 Cat. No.: HY-P1215A

HS024 is a selective MC4 receptor antagonist, HS024 is a selective MC4 receptor antagonist,

with Kis of 0.29, 3.29, 5.45, and 18.6 nM for MC4, with Kis of 0.29, 3.29, 5.45, 18.6 nM for MC4, MC5, MC3, and MC1, respectively. HS024 increase MC5, MC3, and MC1, respectively. HS024 increase food intake. food intake.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg

2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

JKC363 JNJ-10229570 Cat. No.: HY-P1213 Cat. No.: HY-107139

JKC363, a selective melanocortin MC4 receptor JNJ-10229570 is an antagonist of melanocortin antagonist, has a 90-fold higher affinity at the receptor 1 (MC1R) and melanocortin receptor

MC4 receptor (IC50=0.5 nM) than at the MC3 5 (MC5R), which inhibits sebaceous gland receptor (44.9 nM). JKC-363 blocks the stimulatory differentiation and the production of effect of α-MSH on TRH release. Anti-hyperalgesic sebum-specific lipids. effect. Purity: >98% Purity: ≥98.0% Clinical Data: No Development Reported Clinical Data: Phase 1 Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

MC-4R Agonist 1 MK-0493 Cat. No.: HY-U00396 Cat. No.: HY-118930

MC-4R Agonist 1 is an agonist of human MK-0493 is a potent, orally active and selective melanocortin-4 receptor (MC-4R), used in the agonist of the melanocortin receptor 4 research of obesity, diabetes, and sexual (MC4R), demonstrating significant reductions in dysfunction. energy intake.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg

ML-00253764 hydrochloride MSG606 Cat. No.: HY-110123 Cat. No.: HY-P1726

ML-00253764 hydrochloride is a brain penetrant MSG606 is a potent human MC1 receptor antagonist nonpeptidic melanocortin receptor 4 (MC4R) (IC50=17 nM). MSG606 also partial agonist at human antagonist with a Ki and IC50 of 0.16 µM and 0.103 MC3 and MC5 receptors (EC50 values are 59 and µM, respectively. 1300 nM, respectively). MSG606 exhibits binding affinity for A375 melanoma cells in vitro.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg

Neuropeptide EI, rat Nonapeptide-1 acetate salt Cat. No.: HY-P1869 (Melanostatine-5 acetate salt) Cat. No.: HY-P0097A

Neuropeptide EI, rat displays functional melanin Nonapeptide-1 acetate salt, a peptide hormone, is concentrating hormone (MCH)-antagonist and a potent α-Melanocyte-stimulating hormone melanocyte-stimulating hormone (MSH) agonist (α-MSH) antagonist, with an IC50 of 11 nM. activity in different behavioral paradigms. Reduces synthesis of melanin and helps decrease skin pigmentation to a substantial degree.

Purity: >98% Purity: 99.76% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg

PF-00446687 PG-931 Cat. No.: HY-10622 Cat. No.: HY-P1208

PF-00446687 is a potent, selective PG-931, an analog of SHU 9119 (HY-P0227), is a melanocortin-4 receptor (MC4R) agonist with potent melanocortin 4 (MC4) receptor

EC50 of 12±1 nM. Pf-446687 is brain penetrant. (IC50=0.58 nM) agonist and is more selective than

for the hMC3R (IC50=55 nM) or the hMC5R (IC50=2.4 nM). PG-931 can reverse haemorrhagic shock and prevent multiple organ damage in vivo. Purity: 99.78% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg

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PG-931 TFA PG106 Cat. No.: HY-P1208A Cat. No.: HY-P1209

PG-931 TFA, an analog of SHU 9119 (HY-P0227), is a PG106 is a potent and selective human potent melanocortin 4 (MC4) receptor melanocortin 3 (hMC3) receptor antagonist

(IC50=0.58 nM) agonist and is more selective than (IC50=210 nM) and has noactivity

for the hMC3R (IC50=55 nM) or the at hMC4 receptors (EC50=9900 nM)

hMC5R(IC50=2.4 nM). and hMC5 receptor.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg

PG106 TFA RO27-3225 TFA Cat. No.: HY-P1209A Cat. No.: HY-P2242A

PG106 TFA is a potent and selective human RO27-3225 TFA is potent and selective

melanocortin 3 (hMC3) receptor antagonist (IC50= (MC4R) agonist with

210 nM) and has noactivity an EC50 of 1 nM and 8 nM for MC4R and MC1R,

at hMC4 receptors (EC50=9900 nM) respectively. RO27-3225 TFA shows ~30-fold and hMC5 receptor. selectivity for MC4R over MC3R. RO27-3225 TFA has neuroprotective and anti-inflammatory effects. Purity: >98% Purity: 98.97% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg

SHU 9119 SNT-207707 Cat. No.: HY-P0227 Cat. No.: HY-11029

SHU 9119 is a potent human melanocortin 3 and 4 SNT-207707 is a selective, potent and orally receptors (MC3/4R) antagonist and a partial active melanocortin MC-4 receptor antagonist

MC5R agonist; with IC50 values of 0.23, 0.06, with an IC50 of 8 nM (binding) and 5 nM (function) and 0.09 nM for human MC3R, MC4R and MC5R, on the MC-4 receptor. respectively.

Purity: 98.21% Purity: 99.23% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg

SNT-207858 SNT-207858 free base Cat. No.: HY-11030 Cat. No.: HY-11030A

SNT207858 is a selective, blood brain barrier SNT207858 free base is a selective, blood brain penetrating, potent and orally active barrier penetrating, potent and orally active melanocortin-4 (MC-4) receptor antagonist. melanocortin-4 (MC-4) receptor antagonist.

SNT207858 has an IC50 of 22 nM (binding) and 11 nM SNT207858 free base has an IC50 of 22 nM (binding) (function) on the MC-4 receptor. and 11 nM (function) on the MC-4 receptor.

Purity: >98% Purity: 98.06% Clinical Data: No Development Reported Clinical Data: Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg

Terrein THIQ Cat. No.: HY-119808 Cat. No.: HY-10624

Terrein is a melanogenesis inhibitor. Terrein THIQ is the first selective agonist of the induces apoptosis in breast cancer cell lines . melanocortin-4 receptor (MC4R), with high

Terrein is an inhibitor of quorum sensing and affinity and potency for hMC4R (IC50=1.2 nM,

c-di-GMP in Pseudomonas aeruginosa. EC50=2.1 nM) and rMC4R (IC50=0.6 nM, EC50=2.9 nM). THIQ maintains low potency at MC1R, MC3R and MC5R. Purity: >98% Purity: 98.48% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg

4 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

[D-Trp8]-γ-MSH [D-Trp8]-γ-MSH TFA Cat. No.: HY-P1217 Cat. No.: HY-P1217A

[D-Trp8]-γ-MSH is a potent and selective agonist [D-Trp8]-γ-MSH TFA is a potent and selective of melanocortin 3 (MC3) receptor, with IC50s agonist of melanocortin 3 (MC3) receptor, with of 6.7 nM, 600 nM and 340 nM for hMC3, hMC4 IC50s of 6.7 nM, 600 nM and 340 nM for hMC3, and hMC5, respectively in CHO cells. hMC4 and hMC5, respectively in CHO cells.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg

α-Melanocyte-Stimulating Hormone (MSH), α-Melanocyte-Stimulating Hormone (MSH), amide TFA Cat. No.: HY-P0252 Cat. No.: HY-P0252A

α-Melanocyte-Stimulating Hormone (MSH), amide is α-Melanocyte-Stimulating Hormone (MSH), amide TFA an endogenous neuropeptide, with anti-inflammatory is an endogenous neuropeptide, with and antipyretic activities. α-MSH is a anti-inflammatory and antipyretic activities. post-translational derivative of α-MSH is a post-translational derivative of pro-opiomelanocortin (POMC), acts as an endogenous pro-opiomelanocortin (POMC), acts as an endogenous melanocortin receptor 4 (MC4R) agonist. melanocortin receptor 4 (MC4R) agonist. Purity: 98.02% Purity: 99.48% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 25 mg Size: 1 mg, 5 mg, 10 mg, 25 mg

β-Melanocyte Stimulating Hormone (MSH), human β-Melanocyte Stimulating Hormone (MSH), human TFA (Beta-MSH (1-22) (human)) Cat. No.: HY-P1504 (Beta-MSH (1-22) (human) TFA) Cat. No.: HY-P1504A

β-Melanocyte Stimulating Hormone (MSH), human, a β-Melanocyte Stimulating Hormone (MSH), human TFA, 22-residue peptide, acts as an endogenous a 22-residue peptide, acts as an endogenous melanocortin-4 receptor (MC4-R) agonist. melanocortin-4 receptor (MC4-R) agonist.

Purity: >98% Purity: 99.95% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg, 10 mg

γ-1-Melanocyte Stimulating Hormone (MSH), amide γ1-MSH Cat. No.: HY-P1531 Cat. No.: HY-P1214

γ-1-Melanocyte Stimulating Hormone (MSH), amide is γ1-MSH is a melanocortin MC3 receptor agonist, a 11-amino acid peptide. γ-1-Melanocyte with a Ki of 34 nM for the rat MC3 receptor. Stimulating Hormone (MSH) regulates sodium (Na+) γ1-MSH displays ~40-fold selectivity over MC4 balance and through activation of (Ki=1318 nM). the melanocortin receptor 3 (MC3-R).

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 1 mg, 5 mg

γ1-MSH TFA Cat. No.: HY-P1214A

γ1-MSH TFA is a melanocortin MC3 receptor agonist, with a Ki of 34 nM for the rat MC3 receptor. γ1-MSH TFA displays ~40-fold selectivity over MC4 (Ki=1318 nM).

Purity: >98% Clinical Data: No Development Reported Size: 1 mg, 5 mg

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