ELOVL6-IN-1 is a potent, orally active and selective ELOVL6 inhibitor. ELOVL6-IN-1 dose-dependently inhibits mouse ELOVL6 activities, with an IC50 value of 0.350 μM. ELOVL6-IN-1 inhibits ELOVL6 in a noncompetitive manner for malonyl-CoA (Ki=994 nM) and palmitoyl-CoA.
ELOVL6-IN-1 has sufficiently lipophilic having the potential to penetrate the intracellular space in a passive diffusion manner[1].
ELOVL6-IN-1 (10 mg/kg; p.o.; 0~2 hours) displays appreciable plasma and liver exposure[1].
ELOVL6-IN-1 (10 and 30 mg/kg; p.o.; 0~2 hours) reduces the elongation index of the liver lipids[1].
ELOVL6-IN-1 (100 mg/kg; p.o.; 2 days) reduces the elongation index of the total fatty acids of the liver[1].