CAY10566 is a potent and selective stearoyl-CoA desaturase 1 (SCD1) inhibitor (IC50 = 26 nM/hSCD1 and 4.5 nM/mSCD1; IC50 >10 μM/75 receptors, transporters, ion channels). CAY10566 effectively blocks the conversion of saturated long-chain fatty acid-CoAs (LCFA-CoAs) to monounsaturated LCFA-CoAs in HepG2 cells (IC50 = 7.9 nM by C17:1/C17:0 ratio; IC50 = 6.8 nM by C16:1/C16:0 ratio) and exhibits good metabolic stability (by rat & mouse liver microsome assays) and oral availability (rat F = 59.2%; 5 mg/kg p.o.). CAY10566 is typically used in the range from 0.1-10 μM for cell treatment.
Orally available, potent and selective stearoyl-CoA desaturase 1 (SCD1) inhibitor.
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