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 (87):

Cat. No. Product Name Effect Purity
  • 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)[1][2].
  • 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[1][2][3].
  • 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[1][2][3][4].
  • 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[1].
  • 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.
  • HY-P5247A
    Palmitoyl tetrapeptide-20 TFA Activator
    Palmitoyl tetrapeptide-20 (PTP20) TFA is a biomimetic peptide that is an agonist for α-MSH. Palmitoyl tetrapeptide-20 TFA can protect follicular melanocytes and activate melanogenesis by enhancing catalase expression[1].
  • HY-135014
    Undecylenoyl phenylalanine Antagonist
    Undecylenoyl phenylalanine is an antagonist for α-melanocyte-stimulating hormone (MSH) and β-adrenergic receptor (β-ADR) to reduce the melanogenesis in melanocytes, reduces hyperpigmentation and thus ameliorates melasma lesions and solar lentigines[1].
  • HY-158081
    CRN04894 Antagonist
    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[1].
  • HY-N0637A
    (±)-Eriodictyol
    (±)-Eriodictyol ((±)-Huazhongilexone), a flavonoid, is a potent melanogenesis inhibitor with an IC50 of 48 μM. (±)-Eriodictyol suppresses tyrosinase, TRP-1, and TRP-2 mRNA expression. (±)-Eriodictyol has strong anti-plasmin activities[1].
  • HY-110123
    ML-00253764 hydrochloride Inhibitor 99.47%
    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[1].
  • HY-P3645
    (Nle4)-α-MSH Agonist
    (Nle4)-α-MSH is a synthetic analogue of α-MSH (HY-P0252), a melanocyte-stimulating hormone. (Nle4)-α-MSH reversibly darkens frog skins and also exhibits prolonged activity after heat-alkali treatment[1].
  • 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[1].
  • HY-N12267
    N,N′-Diferuloylputrescine Inhibitor
    N,N′-Diferuloylputrescine is a inhibitor of pigmentation with 57% reduction. N,N′-Diferuloylputrescine significantly reduces the protein level of MITF. N,N′-Diferuloylputrescine has strong antioxidant activities as radical scavengers against reactive oxygen species[1].
  • HY-P3561A
    Agouti-related Protein (AGRP) (83-132) Amide (human) (TFA) Inhibitor
    Agouti-related Protein (AGRP) (83-132) Amide (human) TFA is a fragment of agouti-related protein (AGRP) which is a protein found in abundance in the arcuate nucleus of the hypothalamus. AgRP primarily acts as an inverse agonist for the melanocortin-4 receptor (MC4R) to increase food intake[1][2].
  • HY-P3981
    Defensin NP-3A Inhibitor
    Defensin NP-3A (NP-3A; Corticostatin 1) is a human granulocyte peptide, with anti-ACTH activity. Defensins are antimicrobial peptides with and cytotoxic activity[1][2].
  • HY-P3659
    (D-Phe7)-α-MSH
    (D-Phe7)-α-MSH is an α-MSH analogue[1].
  • HY-P1210A
    Lys-γ3-MSH(human) TFA
    Lys-γ3-MSH(human) TFA is a melanocortin peptide derived from the C-terminal of the fragment of pro-opiomelanocortin (POMC). Lys-γ3-MSH(human) TFA potentiates the steroidogenic response of the rat adrenal to adrenocorticotrophin (ACTH). Lys-γ3-MSH(human) TFA is a potent stimulator of lipolysis with an apparent EC50 of 3.56 nM. Lys-γ3-MSH(human) TFA can activate hormone sensitive lipase (HSL) and Perilipin A resulting in lipolysis[1][2].
  • HY-107627
    MCL0020 Antagonist 99.93%
    MCL0020 is a potent and selective melanocortin MC4 receptor antagonist, with an IC50 of 11.63 nM. MCL0020 dose-dependently and significantly attenuates restraint stress-induced anorexia without affecting food intake[1].
  • HY-P2242A
    RO27-3225 TFA Agonist 98.94%
    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[1][2][3].
  • 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[1].