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

Melanocortin Receptor

MC 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 (66):

Cat. No. Product Name Effect Purity
  • HY-P0252
    α-MSH
    Agonist 99.84%
    α-MSH (α-Melanocyte-Stimulating Hormone), an endogenous neuropeptide, is an endogenous melanocortin receptor 4 (MC4R) agonist with anti-inflammatory and antipyretic activities. α-MSH is a post-translational derivative of pro-opiomelanocortin (POMC).
  • HY-P0227
    SHU 9119
    99.87%
    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-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-10624
    THIQ
    Agonist 98.11%
    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-N2466
    Melanotan I
    Agonist
    Melanotan I is a potent non-selective melanocortin receptor (MCR) agonist. Melanotan I is a synthetic analogue of α-melanocyte stimulating hormone (α-MSH) that stimulates melanogenesis. Melanotan I can induce skin tanning by mimicking the actions of a-MSH on the melanocortin type 1 receptors (MC1R) of melanocytes. Melanotan I can be used for sunlight-induced skin cancers research.
  • HY-148349
    PF-07258669
    Antagonist
    PF-07258669 is a melanocortin-4 receptor (MC4) antagonist. PF-07258669 can be used for the research of cachexia, anorexia, or anorexia nervosa.
  • HY-147301
    Resomelagon
    Agonist
    Resomelagon (AP1189) is a potent, orally active melanocortin receptor (MR) agonist about MC1 and MC3. Resomelagon induces ERK1/2 phosphorylation and Ca2+ mobilization. Resomelagon has anti-inflammatory activity. Resomelagon can be used for obesity and chronic inflammation research.
  • HY-18678
    Bremelanotide
    Bremelanotide (PT-141) is an analogue of α-melanocyte-stimulating hormone (α-MSH). Bremelanotide activates the mPOA and other hypothalamic and limbic regions of the brain involved in sexual behavior. Bremelanotide can be used for researching hypoactive sexual desire disorders.
  • HY-10622
    PF-00446687
    Agonist 99.63%
    PF-00446687 is a potent, selective melanocortin-4 receptor (MC4R) agonist with EC50 of 12 ± 1 nM. Pf-446687 is brain penetrant.
  • HY-P0252A
    α-MSH TFA
    Agonist 99.48%
    α-MSH (α-Melanocyte-Stimulating Hormone) TFA, an endogenous neuropeptide, is an endogenous melanocortin receptor 4 (MC4R) agonist with anti-inflammatory and antipyretic activities. α-MSH TFA is a post-translational derivative of pro-opiomelanocortin (POMC).
  • 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-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-P1558
    ACTH (11-24)
    Antagonist
    ACTH (11-24) is an adrenocorticotropic hormone (ACTH) receptor antagonist. ACTH (11-24) is a fragment of adrenocorticotropic and induces cortisol release. ACTH (11-24) can be used for the research of central nervous system.
  • HY-P1216A
    HS014 TFA
    Antagonist 98.81%
    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-P1504A
    β-Melanocyte Stimulating Hormone (MSH), human TFA
    Agonist 99.84%
    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 99.85%
    ACTH (1-17) TFA, an adrenocorticotropin analogue, is a potent human melanocortin 1 (MC1) receptor agonist with a Ki of 0.21 nM.
  • HY-P2242A
    RO27-3225 TFA
    Agonist 98.96%
    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-115644
    BMS-470539 dihydrochloride
    Agonist 99.95%
    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-B1456A
    Fenoprofen
    Agonist 99.72%
    Fenoprofen (LILLY-53858) is a nonsteroidal anti-inflammatory agent (NSAID). Fenoprofen can be used to to relieve symptoms of arthritis (osteoarthritis and rheumatoid arthritis), such as inflammation, swelling, stiffness, and joint pain. Fenoprofen is an allosteric enhancer for melanocortin receptors. Fenoprofen also increases ERK1/2 activation.
  • HY-P0097A
    Nonapeptide-1 acetate salt
    Antagonist
    Nonapeptide-1 (Melanostatine-5) acetate salt, a peptide hormone, is a selective antagonist of MC1R (Ki: 40 nM). Nonapeptide-1 acetate salt is a competitive α-MSH antagonist that potently inhibits intracellular cAMP and melanosome dispersion induced by α-MSH in melanocytes (IC50: 2.5 nM and 11 nM, respectively). Nonapeptide-1 acetate salt inhibits melanin synthesis, and can be used in the research of skin pigmentation and regulation of steroid production in the adrenal gland, skin cancer.