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[1].
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].
[1]. Shimamura K, et al. 5,5-Dimethyl-3-(5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)-1-phenyl-3-(trifluoromethyl)-3,5,6,7-tetrahydro-1H-indole-2,4-dione, a potent inhibitor for mammalian elongase of long-chain fatty acids family 6: examination of its potential utility as a pharmacological tool. J Pharmacol Exp Ther. 2009;330(1):249-256.
