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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 IC50 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 IC50 values of 7.9 and 6.8 nM, respectively, when heptadecanoic acid and palmitic acid are used as the substrate.
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