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

Melanocortin Receptor

MC Receptor

Melanocortin Receptor

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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 Isoform Specific Products:

Melanocortin Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-N7587
    Chlorophorin
    		Inhibitor
    Chlorophorin is a inhibitor of Melanocortin Receptor. Chlorophorin reduces tyrosinase activity and inhibits a-melanocyte-stimulating hormone-induced melanin production in B16F10 melanoma cells.
    Chlorophorin
  • HY-P1210
    Lys-γ3-MSH(human)
    		Agonist
    Lys-γ3-MSH(human) is a melanocortin peptide derived from the C-terminal of the fragment of pro-opiomelanocortin (POMC). Lys-γ3-MSH(human) potentiates the steroidogenic response of the rat adrenal to adrenocorticotrophin (ACTH). Lys-γ3-MSH(human) is a potent stimulator of lipolysis with an apparent EC50 of 3.56 nM. Lys-γ3-MSH(human) can activate hormone sensitive lipase (HSL) and Perilipin A resulting in lipolysis.
    Lys-γ3-MSH(human)
  • HY-P1545
    ACTH (1-17)
    		Agonist
    ACTH (1-17), an adrenocorticotropin analogue, is a potent human melanocortin 1 (MC1) receptor agonist with a Ki of 0.21 nM.
    ACTH (1-17)
  • HY-P1208A
    PG-931 TFA
    		Agonist
    PG-931 TFA, an analog of SHU 9119 (HY-P0227), is a potent melanocortin 4 (MC4) receptor (IC50=0.58 nM) agonist and is more selective than for the hMC3R (IC50=55 nM) or the hMC5R(IC50=2.4 nM). PG-931 TFA can reverse haemorrhagic shock and prevent multiple organ damage in vivo.
    PG-931 TFA
  • HY-P1213A
    JKC363 TFA
    		Antagonist
    JKC363 TFA, a selective melanocortin MC4 receptor antagonist, has a 90-fold higher affinity at the MC4 receptor (IC50=0.5 nM) than at the MC3 receptor (44.9 nM). JKC363 TFA blocks the stimulatory effect of α-MSH on TRH release. Anti-hyperalgesic effect.
    JKC363 TFA
  • HY-P3977
    ACTH (3-24) (human, bovine, mouse, ovine, porcine, rabbit, rat)
    ACTH (3-24) (human, bovine, mouse, ovine, porcine, rabbit, rat) is the 3-24 fragment of adrenocorticotropic hormone (ACTH). ACTH (3-24) (human, bovine, mouse, ovine, porcine, rabbit, rat) can be used for research of a variety of diseases, including cancer, immune diseases, cardiovascular disease.
    ACTH (3-24) (human, bovine, mouse, ovine, porcine, rabbit, rat)
  • HY-P1214A
    γ1-MSH TFA
    		Agonist
    γ1-MSH TFA is a melanocortin MC3 receptor agonist, with a Ki of 34 nM for the rat MC3 receptor. γ1-MSH TFA displays ~40-fold selectivity over MC4 (Ki=1318 nM).
    γ1-MSH TFA
  • HY-119808
    Terrein
    		Inhibitor
    Terrein is a melanogenesis inhibitor. Terrein induces apoptosis in breast cancer cell lines . Terrein is an inhibitor of quorum sensing and c-di-GMP in Pseudomonas aeruginosa.
    Terrein
  • HY-P10571
    GPS1573
    		Antagonist
    GPS1573 is a noncompetitive antagonist of melanocortin type 2 receptor (MC2R) that dose-dependently antagonizes ACTH-stimulated MC2R activity (IC50=66 nM). GPS1573 can be used in the study of Cushing's disease due to its highly selective antagonism of MC2R.
    GPS1573
  • HY-P1726A
    MSG606 TFA
    		Antagonist
    MSG606 TFA is a potent human MC1 receptor antagonist (IC50=17 nM). MSG606 TFA also partial agonist at human MC3 and MC5 receptors (EC50 values are 59 and 1300 nM, respectively). MSG606 TFA exhibits binding affinity for A375 melanoma cells in vitro. MSG606 TFA reverses the induced hyperalgesia in female mice, with no effect in male mice.
    MSG606 TFA
  • 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.
    Bremelanotide
  • HY-153660A
    Bivamelagon hydrochloride
    		Agonist
    MC-4R Agonist 2 hydrochloride (Example 1) is a MC4R agonist. MC-4R Agonist 2 hydrochloride can be used in the study of obesity, diabetes, inflammation, and erectile dysfunction.
    Bivamelagon hydrochloride
  • HY-147301B
    Resomelagon methanesulfonate
    		Agonist
    Resomelagon methanesulfonate (AP1189 methanesulfonate) is the methanesulfonate salt form of Resomelagon (HY-147301). Resomelagon methanesulfonate is an orally active melanocortin receptor (MR) agonist. Resomelagon methanesulfonate induces ERK1/2 phosphorylation and Ca2+ mobilization. Resomelagon methanesulfonate exhibits anti-inflammatory activity in mouse peritonitis and peritonitis model. Resomelagon methanesulfonate can be used for obesity and chronic inflammation research.
    Resomelagon methanesulfonate
  • HY-121764
    MPCI
    		Antagonist
    MPCI is a cell-permeant MC4R-selective ligand with pharmacological chaperone activity. MPCI is a MC4R antagonist with a Ki value of 0.218 μM on HEK293 cells expressing hMC4R. MPCI can be used for the research of MC4R-deficient obesity.
    MPCI
  • HY-U00396
    MC-4R Agonist 1
    		Agonist
    MC-4R Agonist 1 is an agonist of human melanocortin-4 receptor (MC-4R), used in the research of obesity, diabetes, and sexual dysfunction.
    MC-4R Agonist 1
Cat. No. Product Name / Synonyms Application Reactivity
Melanocortin Receptor Isoform Comparison

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