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-P5971
    TCMCB07
    		Antagonist
    TCMCB07, a cyclic nonapeptide peptide, is an orally active and brain-penetrant melanocortin receptor 4 (MC4R) antagonist. TCMCB07 plays an important role in cachexia.
    TCMCB07
  • HY-134046
    (-)-Isodocarpin
    		Inhibitor
    (-)-Isodocarpin (Isodocarpin), a diterpenoid, is a potent melanogenesis inhibitor with an IC50 of 0.19 μM in B16 4A5 cells. (-)-Isodocarpin inhibits the expression of tyrosinase, tyrosine-related protein (TRP)-1, and TRP-2 mRNA.
    (-)-Isodocarpin
  • HY-P1217A
    [D-Trp8]-γ-MSH TFA
    		Agonist
    [D-Trp8]-γ-MSH TFA is a potent and selective agonist of melanocortin 3 (MC3) receptor, with IC50s of 6.7 nM, 600 nM and 340 nM for hMC3, hMC4 and hMC5, respectively in CHO cells. [D-Trp8]-γ-MSH TFA could provide protection against multiple inflammatory disorders such as rheumatoid arthritis and colitis.
    [D-Trp8]-γ-MSH TFA
  • HY-P10265
    Melanostatin, frog
    		Inhibitor
    Melanostatin, frog is an inhibitor for α-melanocyte-stimulating hormone (α-MSH) release, with an IC50 of 60 nM.
    Melanostatin, frog
  • HY-N2466A
    Melanotan I acetate
    		Agonist
    Melanotan I acetate is a potent non-selective melanocortin receptor (MCR) agonist. Melanotan I acetate is a synthetic analogue of α-melanocyte stimulating hormone (α-MSH) that stimulates melanogenesis. Melanotan I acetate can induce skin tanning by mimicking the actions of a-MSH on the melanocortin type 1 receptors (MC1R) of melanocytes. Melanotan I acetate can be used for sunlight-induced skin cancers research.
    Melanotan I acetate
  • HY-P4764
    Ac-(d-Arg)-CEH-(d-Phe)-RWC-NH2
    		Agonist
    Ac-DArg-c[Cys-Glu-His-DPhe-Arg-Trp-Cys]-NH 2 is a cyclic octapeptide with MC4R agonism. Ac-DArg-c[Cys-Glu-His-DPhe-Arg-Trp-Cys]-NH 2 significantly increases heart rate and blood pressure.
    Ac-(d-Arg)-CEH-(d-Phe)-RWC-NH2
  • HY-P3553
    Alsactide
    		Agonist
    Alsactide, a heptadecapeptide analogue, is an adrenocorticotropic hormone (ACTH) agonist. Alsactide can be used in research of central nervous system.
    Alsactide
  • HY-P3561
    Agouti-related Protein (AGRP) (83-132) Amide (human)
    		Antagonist
    Agouti-related Protein (AGRP) (83-132) Amide (human) 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.
    Agouti-related Protein (AGRP) (83-132) Amide (human)
  • HY-155189
    IIIM-8
    		Inhibitor
    IIIM-8 is a melanogenesis inhibitor. IIIM-8 inhibits pigment production both in vitro and in vivo without incurring any cytotoxicity in Human Adult Epidermal Melanocytes (HAEM). IIIM-8 can be used for hyperpigmentation disorders research.
    IIIM-8
  • HY-P0252B
    α-MSH free acid
    		Agonist
    α-MSH free acid (α-Melanocyte-Stimulating Hormone free acid) is an MC3R and MC4R agonist with EC50s of 0.16 nM and 5.6 nM, respectively. α-MSH free acid activates cAMP generation at MC3R and MC4R.
    α-MSH free acid
  • HY-B1456AS
    Fenoprofen-13C6 sodium hydrate
    Fenoprofen-13C6 (sodium hydrate) is the 13C labeled Fenoprofen (HY-B1456A). Fenoprofen 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[1][2][3].
    Fenoprofen-<sup>13</sup>C<sub>6</sub> sodium hydrate
  • 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.
    Undecylenoyl phenylalanine
  • HY-P3567
    (p-Iodo-Phe7)-ACTH (4-10)
    		Antagonist
    (p-Iodo-Phe7)-ACTH (4-10) is a adrenocorticotrophic hormone (ACTH) derivative, which is produced and secreted by the anterior pituitary gland. (p-Iodo-Phe7)-ACTH (4-10) serves as a melanocortin (MC) receptor antagonist and inhibits α-melanocyte-stimulating hormone (α-MSH)-induced excessive grooming behavior in rats.
    (p-Iodo-Phe7)-ACTH (4-10)
  • HY-P5248
    Tetrapeptide-1
    		Agonist
    Tetrapeptide-1 is a bioactive peptide with antioxidant effect and has been reported used as a cosmetic ingredient.
    Tetrapeptide-1
  • HY-B1456AR
    Fenoprofen (Standard)
    		Agonist
    Fenoprofen (Standard) is the analytical standard of Fenoprofen. This product is intended for research and analytical applications. 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.
    Fenoprofen (Standard)
  • HY-153660
    Bivamelagon
    		Agonist
    MC-4R Agonist 2 (Example 1) is a MC4R agonist. MC-4R Agonist 2 can be used in the study of obesity, diabetes, inflammation, and erectile dysfunction.
    Bivamelagon
  • HY-P5247
    Palmitoyl tetrapeptide-20
    		Activator
    Palmitoyl tetrapeptide-20 (PTP20) is a biomimetic peptide that is an agonist for α-MSH. Palmitoyl tetrapeptide-20 can protect follicular melanocytes and activate melanogenesis by enhancing catalase expression.
    Palmitoyl tetrapeptide-20
  • HY-P0097
    Nonapeptide-1
    		Antagonist
    Nonapeptide-1 (Melanostatine-5), a peptide hormone, is a selective antagonist of MC1R (Ki: 40 nM). Nonapeptide-1 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 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
  • 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)
Cat. No. Product Name / Synonyms Application Reactivity
Melanocortin Receptor Isoform Comparison

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