2. シグナル伝達
  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
製品番号 製品名 製品効果 純度 構造式
  • HY-129724A
    α-MSH (11-13) acetate Control 99.31%
    α-MSH (11-13) (ACTH-(11-13)) acetate is a C-terminal tripeptide of α-MSH that can cross the blood-brain barrier. α-MSH (11-13) acetate exhibits antipyretic, anti-inflammatory, and antibacterial activities. α-MSH (11-13) acetate also exerts neuroprotective effects after traumatic brain injury by inhibiting excessive activation of microglia and reducing neuronal apoptosis. α-MSH (11-13) acetate can be used in research related to traumatic brain injury, fever, and bacterial infections.
    α-MSH (11-13) acetate
  • HY-B0288B
    Fenoprofen Calcium hydrate Agonist 99.52%
    Fenoprofen (LILLY-53858) Calcium hydrate is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen Calcium hydrate is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen Calcium hydrate also increases ERK1/2 activation in HEK293T cells. Fenoprofen Calcium hydrate has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis.
    Fenoprofen Calcium hydrate
  • HY-P0252A
    α-MSH TFA Agonist 98.54%
    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-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-18678
    Bremelanotide Agonist 99.69%
    Bremelanotide (PT-141) is a melanocortin receptor agonist. Bremelanotide can activate MC4R and increases dopamine release. Bremelanotide induces appetitive sexual behaviors, female mounting behavior, and repetitive self-grooming. Bremelanotide can be used for the research of hypoactive sexual desire disorders.
    Bremelanotide
  • HY-P1477
    Adrenocorticotropic hormone (1-39), rat Agonist 99.31%
    Adrenocorticotropic hormone (1-39), rat is a potent melanocortin 2 (MC2) receptor agonist.
    Adrenocorticotropic hormone (1-39), rat
  • HY-118930
    MK-0493 Agonist 99.43%
    MK-0493 is an orally active melanocortin-4 receptor (MC4R) agonist. MK-0493 reduces food intake, suppresses weight gain, elevates blood pressure at high doses, and exhibits preclinical erectile regulatory activity. MK-0493 can be used in research related to obesity.
    MK-0493
  • HY-P0060
    Tetracosactide

    テトラコサクチド

    		Agonist 99.46%
    Tetracosactide (Tetracosactrin) is an analogue of adrenocorticotrophic hormone (ACTH). Tetracosactide is the agonist for melanocortin-4 receptor (MC4R) that activates human MC4R with an EC50 of 0.65 nM. Tetracosactide can stimulate the release of corticosteroids such as cortisol from the adrenal gland. Tetracosactide is currently used for the research of ulcerative colitis and Crohn's disease, juvenile/adult rheumatoid arthritis and osteoarthrosis.
    Tetracosactide
  • HY-11030A
    SNT-207858 free base Antagonist 99.66%
    SNT207858 free base is a selective, blood brain barrier penetrating, potent and orally active melanocortin-4 (MC-4) receptor antagonist. SNT207858 free base has an IC50 of 22 nM (binding) and 11 nM (function) on the MC-4 receptor.
    SNT-207858 free base
  • HY-P10571
    GPS1573 Antagonist 99.37%
    GPS1573 is a noncompetitive antagonist of melanocortin type 2 receptor (MC2R) that dose-dependently antagonizes ACTH-stimulated MC2R activity (IC50=66 nM). GPS1573 can be used in the study of Cushing's disease due to its highly selective antagonism of MC2R.
    GPS1573
  • HY-110123
    ML-00253764 hydrochloride Inhibitor 99.29%
    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. ML-00253764 can cross blood-brain barrier.
    ML-00253764 hydrochloride
  • HY-P1504
    β-Melanocyte Stimulating Hormone (MSH), human Agonist 99.80%
    β-Melanocyte Stimulating Hormone (MSH), human, a 22-residue peptide, acts as an endogenous melanocortin-4 receptor (MC4-R) agonist.
    β-Melanocyte Stimulating Hormone (MSH), human
  • HY-P5247
    Palmitoyl tetrapeptide-20 Activator 99.21%
    Palmitoyl tetrapeptide-20 (PTP20) is a biomimetic peptide agonist of α-MSH. Palmitoyl tetrapeptide-20 promotes hair pigmentation and delays hair graying by activating the MC1-R pathway (AC50: 0.16 nM), enhancing catalase activity to reduce H2O2 accumulation, and upregulating SIRT1 activity. Palmitoyl tetrapeptide-20 can be used in research on preventing hair loss and improving hair graying.
    Palmitoyl tetrapeptide-20
  • HY-148349
    PF-07258669 Antagonist 98.44%
    PF-07258669 is an orally active melanocortin-4 receptor (MC4R) antagonist that antagonizes MC4R with an IC50 of 13 nM (Ki=0.46 nM). PF-07258669 can be used for the research of cachexia, anorexia, or anorexia nervosa.
    PF-07258669
  • 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.
    Agouti-related Protein (AGRP) (83-132) Amide (human) TFA
  • HY-P2242A
    RO27-3225 TFA Agonist 98.65%
    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.
    RO27-3225 TFA
  • HY-N0637A
    (±)-Eriodictyol 99.9%
    (±)-Eriodictyol ((±)-Huazhongilexone; Dihydroluteolin) is an orally active TRPV1 receptor antagonist (IC50=44-47 nM, rTRPV1) with antioxidant and anti-inflammatory activities. (±)-Eriodictyol effectively inhibits lipid peroxidation and the release of proinflammatory cytokines by specifically antagonizing the TRPV1 receptor and activating the Nrf2 signaling pathway. (±)-Eriodictyol reduces the levels of ICAM-1, VEGF, eNOS and TNF-α in the retina and maintains the integrity of the blood-retinal barrier. (±)-Eriodictyol alleviates oxidative stress-induced apoptosis and hyperalgesia, enhances the activity and cytotoxicity of immune cells (such as B lymphocytes, NK cells and macrophages), and increases the levels of antioxidant enzymes simultaneously. (±)-Eriodictyol can be used in the research of diabetic retinopathy, acute lung injury and various pain-related diseases.
    (±)-Eriodictyol
  • HY-P0097
    Nonapeptide-1 Antagonist 98.74%
    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-B1456A
    Fenoprofen Agonist 99.70%
    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
  • HY-147301
    Resomelagon Agonist 98.79%
    Resomelagon (AP1189) is a potent, orally active melanocortin receptor (MR) agonist about MC1 and MC3. Resomelagon induces ERK1/2 phosphorylation and Ca2+ mobilization. Resomelagon has anti-inflammatory activity. Resomelagon can be used for obesity and chronic inflammation research.
    Resomelagon
製品番号 製品名 / Synonyms Application Reactivity
Melanocortin Receptor Isoform Comparison

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