Description
Stearoyl-
CoA desaturase (SCD) catalyzes the committed step of the conversion of saturated, long-
chain fatty acids to monounsaturated fatty acids. The SCD1 gene is thought to play a key role in lipid homeostasis and body weight regulation. Thus, modulating SCD1 activity pharmacologically may be a useful tool for regulating type 2 diabetes, dyslipidemia, and obesity. CAY10566 is a potent and selective inhibitor of SCD1 that demonstrates IC
50 values of 4.5 and 26 nM in mouse and human enzymatic assays, respectively. This compound inhibits the conversion of saturated, long-
chain fatty acyl-
CoAs to monounsaturated, long-
chain fatty acyl-
CoAs in HepG2 cells with IC
50 values of 7.9 and 6.8 nM, respectively, when heptadecanoic acid and palmitic acid are used as the substrate.
