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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.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 658.65. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.52 mL||7.59 mL||15.18 mL|
|5 mM||0.3 mL||1.52 mL||3.04 mL|
|10 mM||0.15 mL||0.76 mL||1.52 mL|
|50 mM||0.03 mL||0.15 mL||0.3 mL|
References are publications that support the biological activity of the product.
Vernachio et al (2011) 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. Antimicrob.Agents Chemother. 55 1843 PMID: 21357300
McGuigan et al (2010) Design, synthesis and evaluation of a novel double pro-drug: INX-08189. A new clinical candidate for hepatitis C virus. Bioorg.Med.Chem.Lett. 20 4850 PMID: 20637609
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