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

Melanocortin Receptor

The melanocortin (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 melanocortin receptor (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 melanocortins, 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.

Melanocortin Receptor Related Products (38):

Cat. No. Product Name Effect Purity
  • 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-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-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-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-110123
    ML-00253764 hydrochloride Inhibitor
    ML-00253764 hydrochloride is a brain penetrant nonpeptidic melanocortin receptor 4 (MC4R) antagonist with a Ki and IC50 of 0.16 µM and 0.103 µM, respectively.
  • HY-P1531
    γ-1-Melanocyte Stimulating Hormone (MSH), amide Agonist
    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).
  • HY-P1726
    MSG606 Antagonist
    MSG606 is a potent human MC1 receptor antagonist (IC50=17 nM). MSG606 also partial agonist at human MC3 and MC5 receptors (EC50 values are 59 and 1300 nM, respectively). MSG606 exhibits binding affinity for A375 melanoma cells in vitro. MSG606 reverses morphine-induced hyperalgesia in female mice, with no effect in male mice.
  • 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-P1477A
    Adrenocorticotropic Hormone (ACTH) (1-39), rat TFA Agonist 99.84%
    Adrenocorticotropic Hormone (ACTH) (1-39), rat (TFA) is a potent melanocortin 2 (MC2) receptor 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-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-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-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-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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