1. Signaling Pathways
  2. GPCR/G Protein
    Neuronal Signaling
  3. Melanocortin Receptor

Melanocortin 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).

Melanocortin Receptor Related Products (24):

Cat. No. Product Name Effect Purity
  • HY-19870
    Setmelanotide Agonist 98.67%
    Setmelanotide (RM-493; BIM-22493; IRC-022493) is a selective melanocortin 4 receptor (MC4R) agonist with EC50s of 0.27 nM and 0.28 nM for human and rat MC4R, respectively.
  • HY-18678A
    Bremelanotide Acetate Agonist 99.97%
    Bremelanotide Acetate (PT-141 Acetate), a synthetic peptide analogue of α-MSH, is an agonist at melanocortin receptors including the MC3R and MC4R for the treatment of sexual dysfunction.
  • HY-107139
    JNJ-10229570 Antagonist >98.0%
    JNJ-10229570 is an antagonist of melanocortin receptor 1 (MC1R) and melanocortin receptor 5 (MC5R), which inhibits sebaceous gland differentiation and the production of sebum-specific lipids. JNJ-10229570 inhibits the binding of 125I-NDP-α-MSH to cells expressing human MC1R and MC5R, with IC50 values of 270 nM and 200 nM, respectively.
  • HY-P1504A
    β-Melanocyte Stimulating Hormone (MSH), human TFA Agonist 99.95%
    β-Melanocyte Stimulating Hormone (MSH), human TFA, a 22-residue peptide, acts as an endogenous melanocortin-4 receptor (MC4-R) agonist.
  • HY-10622
    PF-00446687 Agonist 99.78%
    PF-00446687 is a potent, selective melanocortin-4 receptor (MC4R) agonist with EC50 of 12 ± 1 nM. Pf-446687 is brain penetrant.
  • HY-10624
    THIQ Agonist 98.48%
    THIQ is the first selective agonist of the melanocortin-4 receptor (MC4R), with high affinity and potency for hMC4R (IC50=1.2 nM, EC50=2.1 nM) and rMC4R (IC50=0.6 nM, EC50=2.9 nM). THIQ maintains low potency at MC1R, MC3R and MC5R. THIQ plays a role in eliciting erectile activity in rodents. THIQ acts as a pharmacoperone of the MC4R rescuing the cell surface expression and signaling of some intracellularly retained MC4R mutants.
  • HY-115644
    BMS-470539 dihydrochloride Agonist 98.50%
    BMS-470539 dihydrochloride is a highly potent and selective melanocortin-1 receptor (MC-1R) agonist with an IC50 of 120 nM, an EC50 of 28 nM. BMS-470539 dihydrochloride does not activate MC-3R and is a very weak partial agonist at MC-4R and MC-5R. BMS-470539 dihydrochloride has potently anti-inflammatory properties.
  • HY-P2242A
    RO27-3225 TFA Agonist
    RO27-3225 TFA is potent and selective melanocortin 4 receptor (MC4R) agonist with an EC50 of 1 nM and 8 nM for MC4R and MC1R, respectively. RO27-3225 TFA shows ~30-fold selectivity for MC4R over MC3R. RO27-3225 TFA has neuroprotective and anti-inflammatory effects.
  • HY-P1545A
    ACTH (1-17) (TFA) Agonist 99.02%
    ACTH (1-17) TFA, an adrenocorticotropin analogue, is a potent human melanocortin 1 (MC1) receptor agonist with a Ki of 0.21 nM.
  • HY-11030A
    SNT-207858 free base Antagonist 98.06%
    SNT207858 free base is a selective, blood brain barrier penetrating, potent and orally active melanocortin-4 (MC-4) receptor antagonist. SNT207858 free base has an IC50 of 22 nM (binding) and 11 nM (function) on the MC-4 receptor.
  • HY-P1477A
    Adrenocorticotropic Hormone (ACTH) (1-39), rat TFA Agonist 99.25%
    Adrenocorticotropic Hormone (ACTH) (1-39), rat (TFA) is a potent melanocortin 2 (MC2) receptor agonist.
  • HY-P0097A
    Nonapeptide-1 acetate salt Antagonist 99.76%
    Nonapeptide-1 acetate salt, a peptide hormone, is a potent α-Melanocyte-stimulating hormone (α-MSH) antagonist, with an IC50 of 11 nM. Reduces synthesis of melanin and helps decrease skin pigmentation to a substantial degree.
  • HY-11030
    SNT-207858 Antagonist
    SNT207858 is a selective, blood brain barrier penetrating, potent and orally active melanocortin-4 (MC-4) receptor antagonist. SNT207858 has an IC50 of 22 nM (binding) and 11 nM (function) on the MC-4 receptor.
  • HY-P1504
    β-Melanocyte Stimulating Hormone (MSH), human Agonist
    β-Melanocyte Stimulating Hormone (MSH), human, a 22-residue peptide, acts as an endogenous melanocortin-4 receptor (MC4-R) agonist.
  • HY-11029
    SNT-207707 Inhibitor 99.23%
    SNT-207707 is a selective, potent and orally active melanocortin MC-4 receptor antagonist with an IC50 of 8 nM (binding) and 5 nM (function) on the MC-4 receptor.
  • HY-110123
    ML-00253764 hydrochloride Inhibitor
    ML-00253764 is a nonpeptidic melanocortin receptor 4 (MC4R) antagonist with a Ki and IC50 of 0.16 µM and 0.103 µM, respectively. Brain penetrant.
  • HY-P1869
    Neuropeptide EI, rat Agonist
    Neuropeptide EI, rat displays functional melanin concentrating hormone (MCH)-antagonist and melanocyte-stimulating hormone (MSH) agonist activity in different behavioral paradigms.
  • HY-P1477
    Adrenocorticotropic Hormone (ACTH) (1-39), rat Agonist
    Adrenocorticotropic Hormone (ACTH) (1-39), rat is a potent melanocortin 2 (MC2) receptor agonist.
  • HY-P1558
    ACTH (11-24) Antagonist
    ACTH (11-24) is a fragment of adrenocorticotrophin, acts as an antagonist of adrenocorticotropic hormone (ACTH) receptor, and induces cortisol release.
  • HY-19870A
    Setmelanotide TFA Agonist
    Setmelanotide TFA (RM-493 TFA; BIM-22493 TFA; IRC-022493 TFA) is a selective melanocortin 4 receptor (MC4R) agonist with EC50s of 0.27 nM and 0.28 nM for human and rat MC4R, respectively.
Isoform Specific Products

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