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-P0252
    α-MSH
    		Agonist 99.57%
    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).
    α-MSH
  • HY-N2466
    Melanotan I
    		Agonist 99.75%
    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 the research of sun-induced skin cancer, melanoma, inflammation and male erectile dysfunction.
    Melanotan I
  • HY-18678A
    Bremelanotide Acetate
    		Agonist 99.98%
    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.
    Bremelanotide Acetate
  • HY-P0227
    SHU 9119
    		99.95%
    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.
    SHU 9119
  • 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.
    BMS-470539 dihydrochloride
  • HY-148349A
    (2R,2R)-PF-07258669
    		Antagonist
    (2R,2R)-PF-07258669 is a MC4R (melanocortin 4 receptor) antagonist. (2R,2R)-PF-07258669 can be used in the study of regulating appetite and energy expenditure.
    (2R,2R)-PF-07258669
  • HY-109114A
    Dersimelagon phosphate
    		Agonist
    Dersimelagon phosphate is an orally active, selective melanocortin 1 receptor (MC1R) agonist with EC50 values of 8.16, 3.91, 1.14 and 0.251 nM for human (h), cynomolgus monkey (cm), mouse (m) and rat (r) MC1R, respectively. Dersimelagon phosphate shows good affinity for hMC1R and hMC4R with Ki values of 2.26, 32.9 nM, respectively. Dersimelagon phosphate can be used for the research of skin pigmentation.
    Dersimelagon phosphate
  • HY-15616
    BMS-470539
    		Agonist
    BMS-470539 is a synthetic MC-1R agonist with potent anti-inflammatory properties. BMS-470539 selectively activates human and murine MC-1R with EC50 values ??of 16.8 nM and 11.6 nM, respectively. In vitro studies have shown that BMS-470539 is able to dose-dependently inhibit TNF-alpha-induced NF-kB activation in human melanoma cells expressing MC-1R. In vivo, subcutaneous injection of BMS-470539 into BALB/c mice effectively inhibited LPS-induced TNF-alpha production with an ED50 of approximately 10 μmol/kg and a pharmacodynamic half-life of approximately 8 hours. It also significantly reduced leukocyte infiltration in a lung inflammation model and attenuated paw swelling in a delayed-type hypersensitivity model, highlighting its efficacy as an anti-inflammatory agent through MC-1R modulation.
    BMS-470539
  • 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.
    THIQ
  • HY-P0097A
    Nonapeptide-1 acetate salt
    		Antagonist 98.70%
    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.
    Nonapeptide-1 acetate salt
  • 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.
    JNJ-10229570
  • HY-P1726
    MSG606
    		Antagonist 98.25%
    MSG606 is a selective MC1R (melanocortin 1 receptor) antagonist and can be used for the research of neuroprotective effects.
    MSG606
  • HY-P0252A
    α-MSH TFA
    		Agonist 98.79%
    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).
    α-MSH TFA
  • HY-118930
    MK-0493
    		Agonist 99.43%
    MK-0493 is a potent, orally active and selective agonist of the melanocortin receptor 4 (MC4R), demonstrating significant reductions in energy intake.
    MK-0493
  • 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.
    Adrenocorticotropic Hormone (ACTH) (1-39), rat TFA
  • HY-P1215A
    HS024 TFA
    		Antagonist 99.80%
    HS024 is a selective MC4 receptor antagonist, with Kis of 0.29, 3.29, 5.45, 18.6 nM for MC4, MC5, MC3, and MC1, respectively. HS024 increase food intake.
    HS024 TFA
  • HY-109114
    Dersimelagon
    		Agonist 98.66%
    Dersimelagon (MT-7117) is an orally active, selective melanocortin 1 receptor (MC1R) agonist with EC50 values of 8.16, 3.91, 1.14 and 0.251 nM for human (h), cynomolgus monkey (cm), mouse (m) and rat (r) MC1R, respectively. Dersimelagon shows good affinity for hMC1R and hMC4R with Ki values of 2.26, 32.9 nM, respectively. Dersimelagon can be used for the research of skin pigmentation.
    Dersimelagon
  • HY-P1504A
    β-Melanocyte Stimulating Hormone (MSH), human TFA
    		Agonist 99.21%
    β-Melanocyte Stimulating Hormone (MSH), human TFA, a 22-residue peptide, acts as an endogenous melanocortin-4 receptor (MC4-R) agonist.
    β-Melanocyte Stimulating Hormone (MSH), human TFA
  • HY-158081
    Atumelnant
    		Antagonist 98.41%
    CRN04894 (compound 17h) is an orally active MC2R antagonist that demonstrates in vivo efficacy in rat model of adrenocorticotropic hormone (ACTH)-stimulated corticosterone secretion[1]. CRN04894 binds to human or rat MC2R with KB values of 0.34 nM and 0.23 nM, respsectively.
    Atumelnant
  • HY-11029
    SNT-207707
    		Inhibitor 99.51%
    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.
    SNT-207707
Cat. No. Product Name / Synonyms Application Reactivity
Melanocortin Receptor Isoform Comparison

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