Niraparib (R-enantiomer)

Research use only, not for human use.

Niraparib R-enantiomer is an inhibitor of PARP1(IC50 of 2.4 nM).

Niraparib R-enantiomer is an inhibitor of PARP1(IC50 of 2.4 nM).(In Vitro):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 EC50, Niraparib R-enantiomer=30 nM, Niraparib S-enantiomer=4.0 nM; BRCA1-HeLa CC50, Niraparib R-enantiomer=470, Niraparib S-enantiomer=34 nM). .

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 EC50, Niraparib R-enantiomer=30 nM, Niraparib S-enantiomer=4.0 nM; BRCA1-HeLa CC50, Niraparib R-enantiomer=470, Niraparib S-enantiomer=34 nM). Given this improved potency and similar in vitro turnover in human liver microsomes (HLM Clint, Niraparib R-enantiomer=4, Niraparib S-enantiomer=3 μL/min/mgP), Niraparib S-enantiomer (Niraparib) is focused on.

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Niraparib R-enantiomer | MK 4827 (R-enantiomer)

Cell Cycle/DNA Damage

PARP

Farnesyl transferase (FTase)| Parasite

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1038915-58-0

320.396

C19H20N4O

>98% (HPLC)

In Vitro:?DMSO : ≥ 32 mg/mL (99.88 mM)

NC(=O)c1cccc2cn(nc12)-c1ccc(cc1)[C@H]1CCCNC1

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(-20℃)

With Ice Pack

≥ 2 years