Niraparib (R-enantiomer)
规格
Cas Number | 1038915-58-0 |
规格或纯度 | ≥99% |
纯度 | ≥99% |
包装 | 50mg 或 10mg 或 5mg 或 2mg |
产品信息
品牌 | 阿拉丁 |
溶解性 | DMSO : ≥ 32 mg/mL (99.88 mM) |
过滤标签 | 表观遗传学,PARP,Cell Cycle/DNA Damage |
储存温度 | -20°C储存 |
运输条件 | 超低温冰袋运输 |
生化和生理学机理 | 尼拉帕利 R-对映体(MK-4827 R-对映体)是一种出色的 PARP1 抑制剂,IC 50 为 2.4 nM。 |
英文描述 |
Niraparib R-enantiomer (MK-4827 R-enantiomer) is an excellent PARP1 inhibitor with IC 50 of 2.4 nM. In Vitro Niraparib R-enantiomer (MK-4827 R-enantiomer) resolution of Niraparib R-enantiomer give compounds Niraparib R-enantiomer and Niraparib S-enantiomer, both showing excellent inhibition of PARP-1. Niraparib R-enantiomer has somewhat lower in vitro metabolic clearance than the Niraparib S-enantiomer in rat liver microsomes, but Niraparib S-enantiomer is more potent in cell based assays (PARylation EC 50 , Niraparib R-enantiomer=30 nM, Niraparib S-enantiomer=4.0 nM; BRCA1-HeLa CC 50 , Niraparib R-enantiomer=470, Niraparib S-enantiomer=34 nM). Given this improved potency and similar in vitro turnover in human liver microsomes (HLM Cl int , Niraparib R-enantiomer=4, Niraparib S-enantiomer=3 μL/min/mgP), Niraparib S-enantiomer (Niraparib) is focused on. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:PARP-1 2.4 nM (IC 50 ) |