ELOVL6-IN-4 is a potent, selective, and orally active long chain fatty acid elongase 6 (ELOVL6) inhibitor with IC50s of 79 nM and 94 nM for human and mouse ELOVL6, respectively. ELOVL6-IN-4 shows excellent selectivity over the other human ELOVL subtypes (ELOVL1, -2, -3, and -5) and mouse ELOVL3.
ELOVL6-IN-4 (compound 1w) potently reduced the elongation index in mouse hepatocyte cells H2.35, with an IC50 of 30 nM.
ELOVL6-IN-4 (compound 1w; 1-10 mg/kg; oral administration; once) potently and dose-dependently suppresses the elongation index in the liver in mice[1].
References:
[1]. Tsuyoshi Nagase, et al. Synthesis and biological evaluation of a novel 3-sulfonyl-8-azabicyclo[3.2.1]octane class of long chain fatty acid elongase 6 (ELOVL6) inhibitors. J Med Chem. 2009 Jul 23;52(14):4111-4.