BMS 986094
Chemical Name: Neopentyl [[[(2R,3R,4R,5R)-5-(2-amino-6-methoxy-9H-purin-9-yl)-3,4-dihydroxy-4-methyltetrahydrofuran-2-yl]methoxy](naphthalen-1-yloxy)phosphoryl]-L-alaninate
Purity: ≥98%
Biological Activity
Potent hepatitis C virus (HCV) replication inhibitor (EC50 = 35 nM). Is rapidly metabolized in primary human hepatocytes to 2'-C-methyl guanosine triphosphate, an inhibitor of HCV RNA-dependent RNA polymerase NS5b. Displays 10-fold reduction in potency in S282T mutant-expressing versus wild-type replicons. Exhibits synergy with Ribavirin (Cat. No. 4501). Orally bioavailable.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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INX-08189, a phosphoramidate prodrug of 6-O-methyl-2'-C-methyl guanosine, is a potent inhibitor of hepatitis C virus replication with excellent pharmacokinetic and pharmacodynamic properties.
Vernachio et al.
Antimicrob.Agents Chemother., 2011;55:1843 -
Design, synthesis and evaluation of a novel double pro-drug: INX-08189. A new clinical candidate for hepatitis C virus.
McGuigan et al.
Bioorg.Med.Chem.Lett., 2010;20:4850
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