CAY10566 is a potent, orally bioavailable and selective inhibitor of stearoyl-CoA desaturase1 (SCD1) with IC50 of 4.5 and 26 nM in mouse and human enzymatic assays, respectively. It also demonstrates excellent cellular activity in blocking the conversion of saturated long-chain fatty acid-CoAs (LCFA-CoAs) to monounsaturated LCFA-CoAs in HepG2 cells.