Niraparib (R-enantiomer)

SKU: orb1940786

Description

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). .

Key Properties

• CAS Number: 1038915-58-0
• MW: 320.396
• Purity: >98% (HPLC)
• Formula: C₁₉H₂₀N₄O
• SMILES: NC(=O)c1cccc2cn(nc12)-c1ccc(cc1)[C@H]1CCCNC1
• Target: PARP
• Solubility: In Vitro: DMSO : ≥ 32 mg/mL (99.88 mM)

Bioactivity

• 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 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

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

Quick Database Links

Gene Symbol

PARP