CAY10566 is a potent, orally bioavailable and selective stearoyl-CoA desaturase1 ( SCD1 ) inhibitor with IC 50 s of 4.5 and 26 nM in mouse and human enzymatic assays, respectively. CAY10566 also shows excellent cellular activity in blocking the conversion of saturated long-chain fatty acid-CoAs (LCFA-CoAs) to monounsaturated LCFA-CoAs in HepG2 cells (IC 50 =7.9 nM or 6.8 nM).
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