Dersimelagon (C09-1126-353)

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 pigmentationIn VitroDersimelagon (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 VivoDersimelagon (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:SolidIC50& 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 ). Molecular Formula: C36H45F4N3O5 Molecular Weight: 675.75 PubChem CID: 126736894 Isomeric SMILES: COC[C@H]1CN(C[C@@H]1C2=C(C=C(C=C2)C(F)(F)F)N3CCC(CC3)C(=O)O)C(=O)[C@@]4(CN(C[C@H]4C5=CC=C(C=C5)OC)C6CCCC6)F