Dersimelagon  (Synonyms: MT-7117)

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 K_i values of 2.26, 32.9 nM, respectively. Dersimelagon can be used for the research of skin pigmentation^[1][2].

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].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

675.75

C₃₆H₄₅F₄N₃O₅

1835256-48-8

Solid

Off-white to light yellow

O=C(N1C[C@H](C2=C(N3CCC(C(O)=O)CC3)C=C(C(F)(F)F)C=C2)[C@@H](COC)C1)[C@]4([C@H](C5=CC=C(OC)C=C5)CN(C6CCCC6)C4)F

Room temperature in continental US; may vary elsewhere.

• [1]. T. Suzuki, et al. Melanogenic effect of dersimelagon (MT-7117), a novel oral melanocortin 1 receptor agonist. Skin Health Dis. 2022; 2(1):e78.

  [2]. Erwin AL, et al. Porphyrias in the Age of Targeted Therapies. Diagnostics (Basel). 2021;11(10):1795. Published 2021 Sep 29.  [Content Brief]