MK-4827 (R-enantiomer)

Modify Date: 2024-04-04 18:40:30

MK-4827 (R-enantiomer) Structure
MK-4827 (R-enantiomer) structure
Common Name MK-4827 (R-enantiomer)
CAS Number 1038915-58-0 Molecular Weight 320.38800
Density N/A Boiling Point N/A
Molecular Formula C19H20N4O Melting Point N/A
MSDS N/A Flash Point N/A

 Use of MK-4827 (R-enantiomer)


Niraparib R-enantiomer (MK-4827 R-enantiomer) is an excellent PARP1 inhibitor with IC50 of 2.4 nM.

 Names

Name 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide
Synonym More Synonyms

 MK-4827 (R-enantiomer) Biological Activity

Description Niraparib R-enantiomer (MK-4827 R-enantiomer) is an excellent PARP1 inhibitor with IC50 of 2.4 nM.
Related Catalog
Target

PARP-1:2.4 nM (IC50)

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].
References

[1]. Jones P, et al. Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors. J Med Chem. 2009 Nov 26;52(22):7170-85.

 Chemical & Physical Properties

Molecular Formula C19H20N4O
Molecular Weight 320.38800
Exact Mass 320.16400
PSA 72.94000
LogP 3.62050

 Synonyms

2-{4-[(3R)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide
MK-4827 (R-enantiomer)
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