2. シグナル伝達
  3. GPCR/G Protein
    Neuronal Signaling
  4. Melanocortin Receptor
  5. MC4R Isoform

MC4R

MC4R (melanocortin-4 receptor) is a class A G protein-coupled receptor that functions as a central regulator of appetite, energy expenditure, and body-weight homeostasis within the hypothalamic leptin-melanocortin network[1][2]. Activation of proopiomelanocortin (POMC) neurons promotes release of α-melanocyte-stimulating hormone (α-MSH), which activates MC4R signaling and suppresses food intake while increasing energy expenditure, establishing MC4R as a key effector of energy balance regulation[3][1]. Mechanistically, MC4R integrates neuroendocrine signals controlling satiety and metabolic homeostasis, and disruption of MC4R signaling impairs these regulatory processes[2][4]. Disease relevance is strongly supported by human genetics, as MC4R deficiency represents the most common monogenic cause of obesity, and loss-of-function variants are associated with early-onset severe obesity, hyperphagia, and metabolic abnormalities[4][5][6]. In experimental and clinical studies, MC4R pathway dysfunction has therefore become a widely used model for investigating genetic obesity and energy-homeostasis disorders[2][4]. Compared with the closely related melanocortin receptor MC3R, MC4R exhibits a distinct and non-redundant role in body-weight regulation; studies in knockout models indicate that MC3R and MC4R contribute independently and complementarily to energy homeostasis rather than serving interchangeable functions[7]. For experimental applications, selective MC4R agonists, particularly setmelanotide, have demonstrated the ability to restore signaling in subsets of impaired MC4R variants and induce weight loss in MC4R-deficient obesity, supporting their utility as pharmacological tools and therapeutic candidates for melanocortin-pathway research[8][9][10].

References:

MC4R 関連製品 (44):

製品番号 製品名 製品効果 純度
  • HY-P0252
    α-MSH Agonist 99.98%
    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).
  • HY-10624
    THIQ Agonist 98.48%
    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.
  • HY-P0227
    SHU 9119 99.83%
    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-18678A
    Bremelanotide Acetate Agonist 99.97%
    Bremelanotide (PT-141) Acetate is a melanocortin receptor agonist. Bremelanotide Acetate can activate MC4R and increases dopamine release. Bremelanotide Acetate induces appetitive sexual behaviors, female mounting behavior, and repetitive self-grooming. Bremelanotide Acetate can be used for the research of hypoactive sexual desire disorders.
  • HY-153660
    Bivamelagon Agonist 99.50%
    Bivamelagon (MC-4R Agonist 2) is an orally active MC4R agonist with EC50 values of 0.562 nM (Luci assay) and 36.5 nM (cAMP assay), and a Ki of 65 nM. Bivamelagon can be used for the research of diseases such as obesity and diabetes.
  • HY-P11469
    PG-901 Modulator 99.35%
    PG-901 is a full, selective MC5R agonist (EC50 = 0.072 nM for hMC5R). PG-901 is also a full antagonist at the hMC3R and the hMC4R (Kb: 1.0 nM and 0.53 nM, respectively). PG-901 significantly diminishes Cytokines (IL-1α, IL-1β, IL-6). PG-901 increases glucose tolerance, reduces blood glucose, decreases retinal damage.
  • HY-W559510
    MC4R antagonist-3 Antagonist
    MC4R antagonist-3 (example 130) is a MC4R antagonist with affinity for melanocortin receptors.
  • HY-183106
    MC4R antagonist-2 Antagonist
    MC4R antagonist-2 is a potent melanocortin 4 receptor (MC4R) antagonist with an IC50 of 0.54 nM. MC4R antagonist-2 can be used for the research of MC4R-mediated conditions, such as cachexia, osteoporosis, neuropathic pain, depression, hypertension, malnutrition-related obesity, and associated inflammatory diseases.
  • HY-P0097A
    Nonapeptide-1 acetate salt Antagonist
    Nonapeptide-1 (Melanostatine-5) acetate salt, a peptide hormone, is a selective antagonist of MC1R (Ki: 40 nM). Nonapeptide-1 acetate salt 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 acetate salt inhibits melanin synthesis, and can be used in the research of skin pigmentation and regulation of steroid production in the adrenal gland, skin cancer.
  • HY-10622
    PF-00446687 free base Agonist 98.02%
    PF-00446687 is a potent, selective melanocortin-4 receptor (MC4R) agonist with EC50 of 12 ± 1 nM. Pf-446687 is brain penetrant.
  • 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).
  • 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.
  • HY-P0060
    Tetracosactide 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.
  • 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.
  • 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.
  • 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.
  • 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.
  • 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.
  • 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.
  • 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.