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 )
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Niraparib (R-enantiomer)
CAS number：1038915-58-0 molecular formula：C19H20N4O
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compound introduction
Specs
| Chinese alias | 尼拉帕尼(R-对映体) | ||
| English alias | 2-{4-[(3r)-piperidin-3-yl]phenyl}-2h-indazole-7-carboxamide | EX-A2878 | SCHEMBL1422151 | 2-[4-(3R)-3-piperidinylphenyl]-2H-indazole-7-carboxamide | BDBM50316225 | A930243 | MK-4827 R-enantiomer | Niraparib (R-enantiomer) | AKOS030621516 | CHEBI:177299 | | ||
| CAS number | 1038915-58-0 | molecular formula | C19H20N4O |
| molecular weight | 320.39 g/mol | Exact mass | ≥99% |
| PSA | 72.900 Ų | logp | 2.200 |
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