MK-0159

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MK-0159 是一种具有口服活性的和选择性的 CD38 抑制剂，对人、小鼠和大鼠 CD38 的 IC50 分别为 22、3 和 70 nM。MK-0159 对人和啮齿动物的肝脏微粒体也显示出良好的稳定性。MK-0159 增加全血和心脏的 NAD+(烟酰胺腺嘌呤二核苷酸)，降低 ADPR (二磷酸腺苷核糖)。

MK-0159 is an orally active, potent and selective CD38 inhibitor, with IC50 values of 22, 3, and 70 nM for human, mouse and rat CD38, respectively. MK-0159 also shows good microsomal stability for human and rodent liver microsomes. MK-0159 increases NAD+ (nicotinamide adenine dinucleotide) and reduces ADPR (adenosine diphosphate ribose) in whole blood and heart.

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Animal Model:Cardiac I/R injury miceDosage:30 mg/kg Administration:p.o.Result:Reduced infarct size, and the combination of MK-0159 and NAD+ precursor significantly reduced the infarct size compared to MK-0159 alone.Increased whole heart NAD+ levels and decreased ADPR in the heart.

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Others

Other Targets

CD38

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2641484-61-7

400.495

C20H24N4O3S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (249.69 mM; 超声助溶 )

COCCO[C@H]1CC[C@@H](CC1)NC(=O)c1cc(nc2[nH]ccc12)-c1cncs1

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(-20℃)

With Ice Pack

≥ 2 years