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CAS No. : 1835256-48-8
MCE 国际站：Dersimelagon
产品活性：Dersimelagon (MT-7117) 是一种具有口服活性的选择性黑皮质素 1 受体(MC1R) 激动剂，对人 (h)、食蟹猴 (cm)、小鼠 (m) 和大鼠 (r) MC1R 的 EC50 值分别为 8.16、3.91、1.14 和 0.251 nM。Dersimelagon 对 hMC1R 和 hMC4R 表现出良好的亲和力，Ki 值分别为 2.26 和 32.9 nM。Dersimelagon可用于皮肤色素沉着的研究[1][2]。
研究领域：GPCR/G Protein | Neuronal Signaling
In Vitro: Dersimelagon (0, 0.03, 0.1, 0.3, 1, 3, 10, 30, 100, 300 pM; 3 days) increases eumelanin production in a concentration-dependent manner, with EC50 of 13 pM in B16F1 cells[1].
In Vivo: Dersimelagon (0.003, 0.03, 0.3, 3 mg/kg; p.o. for 6 days) induces coat colour darkening in Ay/a mice in 0.3 and 3 mg/kg[1].
Dersimelagon (0.03, 0.3, 3 mg/kg; p.o.; single administration) upregulates the expression of Tyr, Trp1 and Dct of Ay/a mice at 24, 48 and 72 h in the 3 mg/kg[1].
Dersimelagon (1, 3, 10 mg/kg for 4 weeks and 30 mg/kg for 3 weeks; p.o.) induces pigmentation in a dose-dependent manner, and it is reverses after cessation of administration in cynomolgus monkeys[1].
相关产品：Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | GPCR/G Protein Compound Library | Neuronal Signaling Compound Library | Clinical Compound Library | Drug Repurposing Compound Library | Orally Active Compound Library | Anti-Obesity Compound Library | Rare Diseases Drug Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Activators Library | PG106 | Bremelanotide | ACTH (3-24) (human, bovine, mouse, ovine, porcine, rabbit, rat) | ACTH (11-24) | Adrenocorticotropic Hormone (ACTH) (1-39), human(TFA) | MK-0493 | HS024 | Melanotan I acetate | Agouti-related Protein (AGRP) (83-132) Amide (human) | JNJ-10229570 | MCL0020 | MC-4R Agonist 1 | HS014 | [D-Trp8]-γ-MSH | (D-Phe7)-α-MSH | PG-931 | JKC363 | (-)-Isodocarpin | SHU 9119 | Adrenocorticotropic Hormone (ACTH) (1-39), rat | CCZ01048 TFA | β-Melanocyte Stimulating Hormone (MSH), human TFA | RO27-3225 TFA | γ-1-Melanocyte Stimulating Hormone (MSH), amide | ACTH (1-17) (TFA) | Terrein | γ1-MSH TFA
热门产品线：重组蛋白 | 化合物库 | 天然产物 | 荧光染料 | PROTAC | 同位素标记物 | 寡核苷酸 | 抗体 | 点击化学
Trending products：Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides | Antibodies | Click Chemistry
货号: HY-109114
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