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-P11432
    PG-911
    		Modulator
    PG-911 is a full MC5R agonist (EC50 = 0.031 nM for hMC5R). PG-911 is also a full antagonist at the hMC3R and the hMC4R (Kb: 0.38 nM and 0.17 nM, respectively). PG-911 can be used in the research of neurological disorders.
    PG-911
  • HY-N13879
    Amphistin
    		Inhibitor
    Amphistin is a melanogenesis inhibitor found in actinomycete. Amphistin inhibits the melanogenesis of B16 melanoma cells without affecting the growth of the cell.
    Amphistin
  • HY-B0288BR
    Fenoprofen Calcium hydrate (Standard)
    		Agonist
    Fenoprofen (LILLY-53858 (Standard)) (Standard) Calcium hydrate is the analytical standard of Fenoprofen Calcium hydrate (HY-B0288B). This product is intended for research and analytical applications. Fenoprofen 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 Calcium hydrate (Standard)
  • HY-P991221
    ALD1613
    		Antagonist
    ALD1613 is a potent neutralizing monoclonal antibody against adrenocorticotropic hormone (ACTH). ALD1613 neutralizes ACTH-induced signaling and inhibits ACTH-induced cyclic AMP accumulation in a mouse adrenal cell line (Y1) via all five melanocortin receptors. ALD1613 significantly reduces plasma corticosterone levels in wild-type rats. ALD1613 can be used in the study of diseases associated with elevated ACTH levels.
    ALD1613
  • HY-N13922
    Scytalol A
    		Inhibitor
    Scytalol A selectively inhibits biosynthesis of dihydroxynaphthalene melanin in Lachnellula sp. A32-89, but does not inhibit the growth of the strain.
    Scytalol A
  • HY-N14938
    Albocycline K3
    		Inhibitor
    Albocycline K3 is a melanogenesis inhibitor of microbial origin.
    Albocycline K3
  • HY-W738639
    18-Hydroxy-11-deoxy corticosterone
    18-Hydroxy-11-deoxy corticosterone (18-OH-DOC) is a mineralocorticoid whose synthesis is regulated by adrenocorticotropic hormone (ACTH) and angiotensin II. 18-Hydroxy-11-deoxy corticosterone is an intermediate in the metabolism of progesterone and plays an important role in regulating blood pressure and water-salt balance. Continuous infusion of 18-Hydroxy-11-deoxy corticosterone can increase systolic blood pressure in rats, and plasma levels of 18-Hydroxy-11-deoxy corticosterone are significantly elevated in the db/db mouse model of type 2 diabetes, suggesting its potential involvement in metabolic dysregulation and diabetes-related regulation. 18-Hydroxy-11-deoxy corticosterone holds promise for research in areas such as hypertension, diabetes, and other related fields.
    18-Hydroxy-11-deoxy corticosterone
  • HY-N14240
    Melanocin A
    		Inhibitor
    Melanocin A is a Melanin biosynthesis inhibitor. Melanocin A inhibits the biosynthesis of melanin and tyrosinase (IC50 is 9.0 nM, MIC is 0.9 μM). Melanocin A also has antioxidant effect.
    Melanocin A
  • HY-172299
    Delmadinone acetate
    		Inhibitor
    Delmadinone acetate is an orally active compound that can control estrus and ovulation in female and male pets. Delmadinone acetate causes adrenal suppression from inhibition of release of ACTH from the pituitary gland.
    Delmadinone acetate
  • HY-10622R
    PF-00446687 free base (Standard)
    		Agonist
    PF-00446687 free base (Standard) is the analytical standard of PF-00446687 free base (HY-10622). This product is intended for research and analytical applications. PF-00446687 is a potent, selective melanocortin-4 receptor (MC4R) agonist with EC50 of 12 ± 1 nM. Pf-446687 is brain penetrant.
    PF-00446687 free base (Standard)
  • HY-B0288A
    Fenoprofen Calcium
    		Agonist
    Fenoprofen (LILLY-53858) Calcium is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen Calcium is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen Calcium also increases ERK1/2 activation in HEK293T cells. Fenoprofen Calcium has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis.
    Fenoprofen Calcium
  • HY-B1456AR
    Fenoprofen (Standard)
    		Agonist
    Fenoprofen (Standard) (LILLY-53858 (Standard)) is the analytical standard of Fenoprofen (HY-B1456A). This product is intended for research and analytical applications. Fenoprofenc 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 (Standard)
  • HY-107139R
    JNJ-10229570 (Standard)
    		Antagonist
    JNJ-10229570 (Standard) is the analytical standard of JNJ-10229570 (HY-107139). This product is intended for research and analytical applications. 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 (Standard)
  • HY-159909
    ATMW-2
    		Inhibitor
    ATMW-2 is a NeuralGenThesis (NGT)-derived antagonist targeting the melanocortin type 2 receptor (MC2R).
    ATMW-2
  • HY-182773
    MC4R Antagonist-1
    		Antagonist
    MC4R Antagonist-1 (compound 1) is an MC4R-selective antagonist (IC50<10 nM). MC4R Antagonist-1 can be used for the research of cachexia, anorexia, anorexia nervosa, involuntary weight loss, failure to thrive, sarcopenia, muscle wasting, muscle weakness, frailty, osteoporosis.
    MC4R Antagonist-1
  • HY-125055A
    CD08108
    		Agonist
    CD08108 is a selective MC1R full agonist with an EC50 of 70 nM against hMC1R. CD08108 participates in the melanogenesis process. CD08108 promotes cell proliferation. CD08108 can be used in studies related to vitiligo, subcutaneous diseases and photosensitive diseases.
    CD08108
  • 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-N14245
    Melanoxazal
    		Inhibitor
    Melanoxazal is a Melanin biosynthesis inhibitor. Melanoxazal can inhibit melanin formation in the silkworm larva hemolymph (IC50 is 30.1 μg/mL), and also has stronger inhibitory effect against mushroom tyrosinase (IC50 is 4.2 μg/mL), but it has no antimicrobial effect.
    Melanoxazal
  • 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-10624R
    THIQ (Standard)
    		Agonist
    THIQ (Standard) is the analytical standard of THIQ (HY-10624). This product is intended for research and analytical applications. 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 (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
Melanocortin Receptor Isoform Comparison

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