ELOVL6 inhibitor Compound-A is a potent, selective inhibitor of elongase of long-chain fatty acids family 6 (ELOVL6) with IC50 of 169 and 350 nM for human and mouse ELOVL6, respectively.
ELOVL6 inhibitor Compound-A is a potent, selective inhibitor of elongase of long-chain fatty acids family 6 (ELOVL6) with IC50 of 169 and 350 nM for human and mouse ELOVL6, respectively.
Compound-A displays >30-fold selectivity over recombinant human ELOVL family enzymes (ELOVL1, -2, -3, and -5, IC50 values >5-10 uM), also shows negligible or very weak inhibitory effects on rat microsomal SCD, human ACC1 and -2, and human FAS.
Compound-A inhibits ELOVL6 in a noncompetitive manner for malonyl-CoA (Ki=994 nM) and in an uncompetitive manner for palmitoyl-CoA.
Compound-A effectively reduced the elongation index of fatty acids of hepatocytes.
Compound-A (100 mg/kg, oral) significantly reduced the elongation index of the total fatty acids of the liver in mice.
