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MK-8245

CAS No. : 1030612-90-8

MCE 站：MK-8245

产品活性：MK-8245 是一种有效的，肝靶向的硬脂酰 -CoA 去饱和酶 (SCD) 抑制剂，对人 SCD1 和鼠 SCD1 的 IC₅₀ 值分别为 1 nM 和 3 nM，具有抗糖尿病和抗血脂异常的功效。

研究领域：Metabolic Enzyme/Protease

作用靶点：Stearoyl-CoA Desaturase (SCD)

In Vitro: MK-8245 is a potent ａnd liver-specific SCD inhibitor.
MK-8245 displays similar potencies against human, rat ａnd mouse SCD1, with IC₅₀ values of 1 nM for human SCD1 ａnd 3 nM for both rat SCD1 ａnd mouse SCD1.
MK-8245 exhibits a significant SCD inhibition in the rat hepatocyte assay which contains functional, actives organic anion transporting polypeptides (OATPs) with IC₅₀ of 68 nM, while being only weakly active OATPs in the HepG2 cell assay which is devoid of active with IC₅₀ of ~1 μM.

In Vivo: MK-8245 (10mg/kg; p.o.) exhibits a tissue distribution profile concentrated in the liver, with low exposure in tissues associated with potential adverse events in rats, dogs, ａnd rhesus monkeys.
MK-8245 improves glucose clearance in a dose-dependent manner in eDIO mice administrated before the glucose challenge.

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