1. GPCR/G Protein
    Neuronal Signaling
  2. Melanocortin Receptor

Melanocortin Receptor

Melanocortin receptors (MCRs) comprise a family of five, class A, G protein-coupled receptors designated MC1R-MC5R with diverse physiological roles。 MCRs are found in chordates and are regarded as having evolved from a single ancestral receptor, possibly corresponding most closely to MC4R。 Signaling by MCRs has primarily been observed as occurring through the stimulatory α unit Gs which activates adenylyl cyclase to produce cAMP。

The central nervous melanocortin system is involved in energy homeostasis, regulating food intake and energy expenditure. The brain melanocortin system is defined as the primary neurons that express neuropeptide ligands, and secondary neurons expressing the predominant neural melanocortin receptors (MC3R, MC4R). Mutations in the gene encoding melanocortin receptor agonists, or the genes encoding MC3R or MC4R cause obesity. The other members of the melanocortin receptor family are primarily expressed in the periphery, and are involved in regulating pigmentation (MC1R), adrenal gland function (MC2R), immune function (MC1R/MC3R), and sebaceous gland activity (MC5R).

Melanocortin Receptor 相关产品 (12):

Cat. No. Product Name Effect Purity
  • HY-19870
    Setmelanotide Agonist 99.35%
    Setmelanotide (RM-493;BIM-22493;IRC-022493) 是一种黑皮质素4受体 (MC4R) 激动剂,对人类MC4R的EC50值为0.27 nM。
  • HY-18678A
    Bremelanotide Acetate Agonist 99.97%
    Bremelanotide醋酸盐是一种黑皮质素激素受体拮抗剂, 用于治疗性功能障碍。
  • HY-107139
    JNJ-10229570 Antagonist >98.0%
    JNJ-10229570 是肾上腺皮质受体 1 (MC1R) 和肾上腺皮质受体 5 (MC5R) 的拮抗剂,可抑制皮脂腺分化和皮质特异性脂质的产生,其抑制 125I-NDP-α-MSH 和人类细胞中 MC1R 和 MC5R 结合的 IC50 值分别为 270 nM 和 200 nM。
  • HY-P1504
    β-Melanocyte Stimulating Hormone (MSH), human Agonist
    β-Melanocyte Stimulating Hormone (MSH), human是黑皮质素受体 (melanocortin (MC) receptor) 激动剂。
  • HY-P1477A
    Adrenocorticotropic Hormone (ACTH) (1-39), rat TFA Agonist 99.25%
    Adrenocorticotropic Hormone (ACTH) (1-39), rat (TFA) 是一种有效的黑皮质素 2 型受体 (melanocortin 2 receptor, MC2) 激动剂。
  • HY-10622
    PF-00446687 Agonist
    PF-00446687 是一种有效的,脑渗透性的,选择性黑皮质素 4 受体 (MC4R) 激动剂,EC50 为 12 ± 1 nM。
  • HY-P1545
    ACTH 1-17 Agonist
    ACTH (1-17) 是促肾上腺皮质激素类似物,是一种有效的人黑皮素受体 (human melanocortin 1 (MC1) receptor) 激动剂,Ki 值为0.21 nM。
  • HY-P1531
    γ-1-Melanocyte Stimulating Hormone (MSH), amide Agonist
    γ-1-Melanocyte Stimulating Hormone (MSH), amide 是一种含 11 个氨基酸的多肽。γ-1-Melanocyte Stimulating Hormone 通过激活黑皮质素受体 3 (MC3-R) 来调节钠 (Na+) 平衡和血压。
  • HY-P1477
    Adrenocorticotropic Hormone (ACTH) (1-39), rat Agonist
    Adrenocorticotropic Hormone (ACTH) (1-39), rat 是一种有效的黑皮质素 2 型受体 (melanocortin 2 receptor, MC2) 激动剂。
  • HY-11030
    SNT-207858 Antagonist
    SNT-207858是一种选择性,有口服活性的黑皮质素 (melanocortin MC-4) 受体拮抗剂,选择性分别是MC-3和MC-5的170和40倍。 SNT-207858对MC-4受体的IC50 值为8 nM (结合) and 5 nM (功能)。
  • HY-11029
    SNT-207707 Inhibitor
    SNT-207707是一种有效,选择性,有口服活性的黑素皮质素受体 (melanocortin MC-4) 拮抗剂,IC50 值为8 nM (结合) 和5 nM (功能)。
  • HY-U00396
    MC-4R Agonist 1 Agonist
    MC-4R Agonist 1 是一种黑素皮质素受体 4 (human melanocortin-4 receptor) 的激动剂,可用于肥胖、糖尿病及性功能紊乱等疾病的研究。
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