|VX-222 (VCH-222, Lomibuvir)NNI of HCV RNA polymerase|
Sample solution is provided at 25 µL, 10mM.
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|Description||VX-222 is a potent and selective inhibitor of HCV RNA-dependent RNA polymerase with IC50 value of 0.94-1.2 μM.|
|Targets||HCV RNA-dependent RNA polymerase|
|Cas No.||1026785-59-0||SDF||Download SDF|
|Synonyms||Lomibuvir, VCH222,VCH-222, VX222|
|Chemical Name||5-(3,3-dimethylbut-1-ynyl)-3-[(4-hydroxycyclohexyl)-(4-methylcyclohexanecarbonyl)amino]thiophene-2-carboxylic acid|
|Solubility||Soluble in DMSO > 10 mM||Storage||Store at -20°C|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
|Shipping Condition||Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
VX-222, a derivative of thiophene-2-carboxylic acid, is a potent non-nucleoside inhibitor (NNI) of the hepatitis C virus (HCV) RNA polymerase, an enzyme regulating RNA synthesis by a de novo-initiated mechanism or by extension from a primed template, that binds to the thumb II allosteric pocket of HCV RNA-dependent RNA polymerase with hydrophobical interactions between the 4-methycyclohexanoyl group of VX-222 and L412, M423 and I482 of thumb II domain. VX-222 exhibits preferential inhibition against primer-dependent RNA synthesis rather than de novo-initiated RNA synthesis with 50% inhibition concentration IC50 values ranging from 0.011 to >5 μM in five different templates of RNA synthesis.
Yi G, Deval J, Fan B, Cai H, Soulard C, Ranjith-Kumar CT, Smith DB, Blatt L, Beigelman L, Kao CC. Biochemical study of the comparative inhibition of hepatitis C virus RNA polymerase by VX-222 and filibuvir. Antimicrob Agents Chemother. 2012 Feb;56(2):830-7. doi: 10.1128/AAC.05438-11. Epub 2011 Dec 5.