产品
编 号：F013973
分子式：C17H16BrFN6O4
分子量：467.25
分子式：C17H16BrFN6O4
分子量：467.25
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
2mg
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5mg
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10mg
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50mg
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结构图
CAS No: 1030612-90-8
产品详情
生物活性：
MK-8245 is a potent, liver-targeted stearoyl-CoA desaturase (SCD) inhibitor, with IC50s of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with antidiabetic and antidyslipidemic efficacy.
体内研究：
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.Animal Model:Male C57BL6 mice, male Sprague-Dawley rats
Dosage:10mg/kg
Administration:Oral administration
Result:Exhibits a tissue distribution profile concentrated in the liver.
体外研究：
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.
MK-8245 is a potent, liver-targeted stearoyl-CoA desaturase (SCD) inhibitor, with IC50s of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with antidiabetic and antidyslipidemic efficacy.
体内研究：
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.Animal Model:Male C57BL6 mice, male Sprague-Dawley rats
Dosage:10mg/kg
Administration:Oral administration
Result:Exhibits a tissue distribution profile concentrated in the liver.
体外研究：
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.
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