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-123106
    MCL-0129
    		Antagonist
    MCL-0129 is a compound with anxiolytic and antidepressant activity and is a selective MC4 receptor antagonist that exhibits anxiolytic and antidepressant-like behaviors in multiple rodent models.
    MCL-0129
  • HY-RS08206
    MC3R Human Pre-designed siRNA Set A
    		Inhibitor

    MC3R Human Pre-designed siRNA Set A contains three designed siRNAs for MC3R gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    MC3R Human Pre-designed siRNA Set A
  • HY-129724
    α-MSH (11-13)
    		Control
    α-MSH (11-13) (ACTH-(11-13)) is the 11-13 amino acid (lysine-proline-valine) sequence of α-MSH (HY-P0252), which reduces fever in rabbits.
    α-MSH (11-13)
  • 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-RS08202
    MC1R Rat Pre-designed siRNA Set A
    		Inhibitor

    MC1R Rat Pre-designed siRNA Set A contains three designed siRNAs for MC1R gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    MC1R Rat Pre-designed siRNA Set A
  • 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-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-P11293
    DOTA-GGNle-CycMSHhex
    DOTA-GGNle-CycMSHhex is a melanocortin-1 receptor (MC1R)-targeting peptide that can be radionuclide-labeled for melanoma imaging.
    DOTA-GGNle-CycMSHhex
  • 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-P4985
    γ3-MSH
    γ3-MSH is derived from the N-terminal segment of pro-opiomelanocortin (POMC). γ3-MSH stimulates aldosterone secretion by human adrenal tumor cells in culture.
    γ3-MSH
  • 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
    		Agonist
    Fenoprofen-13C6 (LILLY-53858-13C6) sodium hydrate is the 13C labeled Fenoprofen (HY-B1456A).Fenoprofen (LILLY-53858) is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen also increases ERK1/2 activation in HEK293T cells. Fenoprofen has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis.
    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-P6176
    JLB2-110c
    		Inhibitor
    JLB2-110c activates MCRs receptor (mMC4R EC50 = 0.34 nM) and has a strong in vivo appetite suppressant effect.
    JLB2-110c
  • 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-P2113
    ORG-2766
    ORG-2766 is an adrenocorticotropic hormone ACTH 4-9 analog and neurotrophic peptide. ORG-2766 affects behavioral processes such as memory and attention in animals, improving symptoms in rats with experimental allergic neuritis. ORG-2766 has a neuroprotective effect.
    ORG-2766
  • HY-P10985
    CTX-1211
    		Agonist
    CTX-1211 is a selective, orally effective melanocortin MC4R agonist (EC50=0.38 nM). CTX-1211 can enhance the feeding suppression and weight loss effects induced by liraglutide (HY-P0014), and promote anorexia and weight loss activity. CTX-1211 is mainly used in the study of obesity and other metabolic disorders.
    CTX-1211
Cat. No. Product Name / Synonyms Application Reactivity
Melanocortin Receptor Isoform Comparison

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