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抑制剂描述:

产品名称:INO-1001

产品别名:见爱必信

英文别名:INO-1001

靶点:PARP

CAS:3544-24-9

纯度:>98%

外观:见爱必信

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

INO-1001是一种有效的PARP抑制剂,作用于CHO细胞的IC50为<50 nM,在再灌注期间,是一种因氧化诱导而发生的心肌功能障碍的调节剂。用浓度为0.05 到50 μM的INO-1001处理CHO细胞30分钟,明显抑制PARP 活性, IC50 为50 nM, INO-1001浓度为1 μM 或更高时抑制PARP活性达95%,且没有细胞毒性。此外, INO-1001通过阻断大部分受辐射的核酸片段修复而使CHO 细胞敏感。用400 μM H2O2处理后,通过增强乙酰胆碱诱导的, 依赖内皮细胞层的, NO调节的血管舒张,而提高INO-1001抑制PARP活性。

溶解性:Ethanol :26 mg/mL (191 mM)
DMSO :26 mg/mL (191 mM)

体外研究:

INO-1001 (>1 μM) leads to more than 95% inhibition of PARP activity without significant cellular toxicity. In addition, INO-1001 significantly sensitizes CHO cells by blocking most of the DNA repair occurring between radiation fractions. Inhibition of PARP activity by INO-1001 significantly improves endothelial function by enhancing the acetylcholine-induced, endothelium-dependent, nitric oxide mediated vasorelaxation after exposure with 400 μM H2O2.

体内研究:In a db/db (Leprdb/db) mouse model, INO-1001 ameliorates diabetes-induced albumin excretion and mesangial expansion, and also decreases diabetes-induced podocyte depletion. Treatment with INO-1001 (1.6 mg/kg via intracerebral injection) prevents NAD+ depletion and improves water maze performance after controlled cortical impact (CCI) in mice.

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