Dersimelagon

Research use only, not for human use.

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 (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