产品
编 号：F754245
分子式：C20H24N4O3S
分子量：400.49
分子式：C20H24N4O3S
分子量：400.49
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
50mg
询价
询价
结构图
CAS No: 2641484-61-7
产品详情
生物活性：
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.
体内研究：
MK-0159 (3-30 mg/kg，口服，单剂量) 可增加小鼠血液和心脏中的全身 NAD+ 并降低 ADPR 水平 (CD38 酶活性的产物和底物)。MK-0159 (30 mg/kg，口服) 可减少心脏 I/R 损伤小鼠的梗塞面积。MK-0159 (30 mg/kg，口服灌胃，每天两次，持续 9 天) 可逆转 LCMV 感染的 BXD2 狼疮易发小鼠的线粒体缺陷，恢复 CD8+ T 细胞功能并抑制病毒诱导的器官炎症。Animal Model:Cardiac I/R injury mice
Dosage: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.
体外研究：
MK-0159 (Compound 37) (0-50 μM，24 小时)可增加 A549 细胞和 HMVEC 细胞的细胞外和细胞内 NAD+。MK-0159 (20 μM，过夜) 可减少 CD38 过表达 CD8+ T 细胞中线粒体受损的细胞数量。
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.
体内研究：
MK-0159 (3-30 mg/kg，口服，单剂量) 可增加小鼠血液和心脏中的全身 NAD+ 并降低 ADPR 水平 (CD38 酶活性的产物和底物)。MK-0159 (30 mg/kg，口服) 可减少心脏 I/R 损伤小鼠的梗塞面积。MK-0159 (30 mg/kg，口服灌胃，每天两次，持续 9 天) 可逆转 LCMV 感染的 BXD2 狼疮易发小鼠的线粒体缺陷，恢复 CD8+ T 细胞功能并抑制病毒诱导的器官炎症。Animal Model:Cardiac I/R injury mice
Dosage: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.
体外研究：
MK-0159 (Compound 37) (0-50 μM，24 小时)可增加 A549 细胞和 HMVEC 细胞的细胞外和细胞内 NAD+。MK-0159 (20 μM，过夜) 可减少 CD38 过表达 CD8+ T 细胞中线粒体受损的细胞数量。
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