Dersimelagon

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

Dersimelagon (MT-7117) is an orally active, selective melanocortin 1 receptor (MC1R) agonist with EC50 values of 8.16, 3.91, 1.14 and 0.251 nM for human (h), cynomolgus monkey (cm), mouse (m) and rat (r) MC1R, respectively. Dersimelagon shows good affinity for hMC1R and hMC4R with Ki values of 2.26, 32.9 nM, respectively. Dersimelagon can be used for the research of skin pigmentation.

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.

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.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.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.Animal Model:Cynomolgus monkeys Dosage:1, 3, 10, 30 mg/kg Administration:P.o.; 1, 3, 10 mg/kg for 4 weeks and 30 mg/kg for 3 weeks Result:Induced pigmentation in a dose-dependent manner.Minimum pigmentation effective dose was 1 mg/kg.Pigmentation diminished 4 weeks after cessation of treatment in the 1, 3 and 10 mg/kg groups and 16 weeks after cessation in the 30 mg/kg group.

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GPCR/G Protein

Melanocortin Receptor

Melanocortin Receptor

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1835256-48-8

675.75

C36H45F4N3O5

>98% (HPLC)

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C(=O)([C@@]1(F)[C@@H](CN(C1)C2CCCC2)C3=CC=C(OC)C=C3)N4C[C@@H]([C@@H](COC)C4)C5=C(C=C(C(F)(F)F)C=C5)N6CCC(C(O)=O)CC6

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(-20℃)

With Ice Pack

≥ 2 years