Niraparib (R-enantiomer)
CAS No. : 1038915-58-0
(Synonyms: MK 4827 (R-enantiomer))
| Size | Price | Stock |
|---|---|---|
| 5mg | $86 | In-stock |
| 10mg | $120 | In-stock |
| 50mg | $216 | In-stock |
| 100mg | $336 | In-stock |
| 500mg | $816 | In-stock |
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| 5 g | Get quote | |
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| Cat. No. : | HY-10619D |
| M.Wt: | 320.39 |
| Formula: | C19H20N4O |
| Purity: | >98 % |
| Solubility: | DMSO : ≥ 32 mg/mL |
Niraparib R-enantiomer (MK-4827 R-enantiomer) is an excellent PARP1 inhibitor with IC50 of 2.4 nM. IC50 & Target: IC50: 2.4 nM (PARP1)[1] 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[1].
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