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 (33):

Cat. No. Product Name Effect Purity
  • HY-19870
    Setmelanotide Agonist 98.67%
    Setmelanotide (RM-493) 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-P0252
    α-Melanocyte-Stimulating Hormone (MSH), amide Agonist 98.02%
    α-Melanocyte-Stimulating Hormone (MSH), amide is an endogenous neuropeptide, with anti-inflammatory and antipyretic activities. α-MSH is a post-translational derivative of pro-opiomelanocortin (POMC), acts as an endogenous melanocortin receptor 4 (MC4R) agonist.
  • 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-P0227
    SHU 9119 98.21%
    SHU 9119 is a potent human melanocortin 3 and 4 receptors (MC3/4R) antagonist and a partial MC5R agonist; with IC50 values of 0.23, 0.06, and 0.09 nM for human MC3R, MC4R and MC5R, respectively.
  • HY-19870B
    Setmelanotide acetate Agonist 99.89%
    Setmelanotide acetate (RM-493 acetate) 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-P1215
    HS024 Antagonist
    HS024 is a selective MC4 receptor antagonist, with Kis of 0.29, 3.29, 5.45, and 18.6 nM for MC4, MC5, MC3, and MC1, respectively. HS024 increase food intake.
  • HY-P1216A
    HS014 TFA Antagonist
    HS014 TFA is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors respectively. HS014 TFA modulates the behavioral effects of morphine in mice. HS014 TFA increases food intake in free-feeding rats.
  • 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-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-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-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-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-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-P2242A
    RO27-3225 TFA Agonist 98.97%
    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-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-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-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.
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