Dersimelagon (MT-7117) is an orally active, selective melanocortin 1 receptor ( MC1R ) agonist with EC 50 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 K i values of 2.26, 32.9 nM, respectively. Dersimelagon can be used for the research of skin pigmentation
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 EC 50 of 13 pM in B16F1 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 . 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.
Form:Solid
IC50& Target:hMC1R 2.26 nM (Ki) hMC4R 32.9 nM (Ki) hMC5R 486 nM (Ki) hMC3R 1420 nM (Ki) hMC1R 8.16 nM (EC 50 ) hMC4R 79.6 nM (EC 50 ) hMC2R >10000 nM (EC 50 ) rMC1R 0.251 nM (EC 50 ) mMC1R 1.14 nM (EC 50 ) cmMC1R 3.91 nM (EC 50 )
