MK8245

Описание

MK-8245 is a liver-targeted inhibitor of stearoyl-CoA desaturase (SCD; IC₅₀s = 3, 3, and 1 nM for rat, mouse, and human SCD1, respectively). It is selective for SCD1 over Δ⁵- and Δ⁶-desaturases (IC₅₀s = >100,000 nM). MK-8245 (20-60 mg/kg) reduces the hepatic, but not Harderian gland, ratio of oleic acid to stearic acid, a marker of chronic SCD activity, and blood glucose levels, without inducing the formation of skin lesions or eye squinting behavior, in a mouse model of high-fat diet-induced obesity. It also inhibits hepatitis C virus (HCV) replication without inducing cytotoxicity in LucNeo2 cells (IC₅₀ = 39.8 nM).

Использование

This product is Informer compound X9 of the Aryl Halide Chemistry Informer Library developed by chemists at Merck & Co., Inc., Kenilworth, NJ, U.S., which contains 18 drug-like molecules representative of those encountered in complex synthesis. By screening a new reaction against the Informer Library, chemists can directly compare and analyse a reaction′s successes and shortcomings among different methods and various research teams. It may also be used to facilitate deeper method development for performance or utility.