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MK-8245

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Chemical Structure| 1030612-90-8 同义名 : -
CAS号 : 1030612-90-8
货号 : A515360
分子式 : C17H16BrFN6O4
纯度 : 99%+
分子量 : 467.249
MDL号 : MFCD20039622
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(224.72 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

1% CMC+0.5% Tween-80+water 30 mg/mL suspension

生物活性
靶点

  • Dehydrogenase

    SCD1 (rat), IC50:3 nM

    SCD1 (mouse), IC50:1 nM
描述 Stearoyl-CoA desaturase (SCD) is conserved in all eukaryotes and introduces the first double bond into saturated fatty acyl-CoAs which makes it pivotal in fatty acid metabolism[2]. MK-8245 is a potent, liver-targeted SCD inhibitor, with IC50s of 1 nM for human SCD1 and 3 nM for both rat 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. 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 established diet-induced obese (eDIO) mice administrated before the glucose challenge[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.14mL

0.43mL

0.21mL

10.70mL

2.14mL

1.07mL

21.40mL

4.28mL

2.14mL
参考文献

[1]Oballa RM, Belair L, et al. Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia. J Med Chem. 2011 Jul 28;54(14):5082-96.

[2]Bai Y, McCoy JG, Levin EJ, et al. X-ray structure of a mammalian stearoyl-CoA desaturase. Nature. 2015;524(7564):252-256.

[3]Oballa RM, Belair L, Black WC, et al. Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia. J Med Chem. 2011;54(14):5082-5096.