Melanocortin Receptor MC Receptor

Melanocortin receptors (MCRs) comprise a family of five, class A, G protein-coupled receptors designated MC1R-MC5R with diverse physiological roles. MCRs are found in chordates and are regarded as having evolved from a single ancestral receptor, possibly corresponding most closely to MC4R. Signaling by MCRs has primarily been observed as occurring through the stimulatory α unit Gs which activates adenylyl cyclase to produce cAMP. The central nervous melanocortin system is involved in energy homeostasis, regulating food intake and energy expenditure. The brain melanocortin system is defined as the primary neurons that express neuropeptide ligands, and secondary neurons expressing the predominant neural melanocortin receptors (MC3R, MC4R). Mutations in the gene encoding melanocortin receptor agonists, or the genes encoding MC3R or MC4R cause obesity. The other members of the melanocortin receptor family are primarily expressed in the periphery, and are involved in regulating pigmentation (MC1R), adrenal gland function (MC2R), immune function (MC1R/MC3R), and sebaceous gland activity (MC5R).

www.MedChemExpress.com 1 Melanocortin Receptor Inhibitors & Modulators

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

Bioactivity: ACTH (1-17) TFA, an adrenocorticotropin analogue, is a potent Bioactivity: ACTH (1-17), an adrenocorticotropin analogue, is a potent

human melanocortin 1 (MC1) receptor agonist with a Ki of human melanocortin 1 (MC1) receptor agonist with a Ki of 0.21 nM. 0.21 nM.

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, 10 mg

Adrenocorticotropic Hormone (ACTH) (1-39), rat Adrenocorticotropic Hormone (ACTH) (1-39), rat TFA (ACTH (1-39) (mouse, rat)) Cat. No.: HY-P1477 (ACTH (1-39) (mouse, rat) (TFA)) Cat. No.: HY-P1477A

Bioactivity: Adrenocorticotropic Hormone (ACTH) (1-39), rat is a potent Bioactivity: Adrenocorticotropic Hormone (ACTH) (1-39), rat (TFA) is a melanocortin 2 (MC2) receptor agonist. potent melanocortin 2 (MC2) receptor agonist.

Purity: >98% Purity: 99.25% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 500u g, 1 mg, 5 mg Size: 10mM x 1mL in Water, 500u g, 1 mg, 5 mg

Bremelanotide Acetate JNJ-10229570 (PT-141 Acetate) Cat. No.: HY-18678A Cat. No.: HY-107139

Bioactivity: Bremelanotide Acetate is a melanocortin agonist. IC50 value: Bioactivity: JNJ-10229570 is an antagonist of melanocortin receptor 1 Target: melanocortin in vivo: Bremelanotide is a novel drug (MC1R) and melanocortin receptor 5 (MC5R), which candidate for the treatment of male and female sexual inhibits sebaceous gland differentiation and the production of dysfunction. Bremelanotide has shown promise in effectively sebum-specific lipids. JNJ-10229570 inhibits the binding of treating erectile dysfunction (ED) without the cardiovascular… 125I-NDP-α-MSH to cells expressing human MC1R and MC5R,… Purity: 99.97% Purity: 98.0% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

MC-4R Agonist 1 Nonapeptide-1 acetate salt Cat. No.: HY-U00396 (Melanostatine-5 acetate salt) Cat. No.: HY-P0097A

Bioactivity: MC-4R Agonist 1 is an agonist of human melanocortin-4 Bioactivity: Nonapeptide-1 acetate salt, a peptide hormone, is a potent receptor (MC-4R), used in the research of obesity, α-Melanocyte-stimulating hormone (α-MSH) antagonist, with

diabetes, and sexual dysfunction. an IC50 of 11 nM. Reduces synthesis of melanin and helps decrease skin pigmentation to a substantial degree [1]. Purity: >98% Purity: 99.76% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg

PF-00446687 Setmelanotide Cat. No.: HY-10622 (RM-493; BIM-22493; IRC-022493) Cat. No.: HY-19870

Bioactivity: PF-00446687 is a potent, selective melanocortin-4 receptor Bioactivity: Setmelanotide (RM-493;BIM-22493;IRC-022493) is a [1] ( MC4R) agonist with EC50 of 12±1 nM . Pf-446687 is melanocortin 4 receptor ( MC4R) agonist with an EC50 of brain penetrant [2]. 0.27 nM for human MC4R.

Purity: >98% Purity: 99.35% Clinical Data: No Development Reported Clinical Data: Launched Size: 250 mg, 500 mg Size: 10mM x 1mL in Water, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

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

SNT-207707 SNT-207858 Cat. No.: HY-11029 Cat. No.: HY-11030

Bioactivity: SNT-207707 is a selective, potent and orally active Bioactivity: SNT-207858 is a selective and orally available melanocortin

melanocortin MC-4 receptor antagonist with an IC50 of 8 MC-4 receptor antagonist with a 170-fold selectivity vs. nM (binding) and 5 nM (function) on the MC-4 receptor. MC-3 and a 40-fold selectivity versus MC-5. SNT-207858 has an IC50 of 8 nM (binding) and 5 nM (function) on the MC-4 receptor. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 250 mg, 500 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

Bioactivity: β-Melanocyte Stimulating Hormone (MSH), human, a 22-residue Bioactivity: β-Melanocyte Stimulating Hormone (MSH), human TFA, a peptide, acts as an endogenous melanocortin-4 receptor ( 22-residue peptide, acts as an endogenous melanocortin-4 MC4-R) agonist [1]. receptor ( MC4-R) agonist [1].

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

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

Bioactivity: γ-1-Melanocyte Stimulating Hormone (MSH), amide is a 11-amino acid peptide. γ-1-Melanocyte Stimulating Hormone (MSH) regulates sodium (Na +) balance and blood pressure through activation of the melanocortin receptor 3 ( MC3-R).

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