ELOVL6-IN-1 is a potent, orally active, and selective ELOVL6 inhibitor that dose-dependently inhibits mouse ELOVL6 activities with an IC50 value of 0.350 μM. It inhibits ELOVL6 in a noncompetitive manner for malonyl-CoA (Ki=994 nM) and palmitoyl-CoA[1].

ELOVL6:0.35 μM, ELOVL6:994 nM(ki)

ELOVL6-IN-1 has sufficiently lipophilic. It has the potential to penetrate the intracellular space in a passive diffusion manner potentially[1].

ELOVL6-IN-1 (10 mg/kg; p.o.; 0~2 hours) shows significant plasma and liver exposure[1]. At doses of 10 and 30 mg/kg (p.o.; 0~2 hours), it reduces the elongation index of liver lipids[1]. Additionally, a dose of 100 mg/kg (p.o.; 2 days) decreases the elongation index of total liver fatty acids[1].