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VX-222 (VCH-222, Lomibuvir)NNI of HCV RNA polymerase

VX-222 (VCH-222, Lomibuvir)

Catalog No. A4032
Size Price Stock Qty
5mg $110.00 In stock
10mg $200.00 In stock
50mg $590.00 In stock
100mg $960.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

VX-222

Biological Activity

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          
IC50 0.94-1.2 μM          

VX-222 (VCH-222, Lomibuvir) Dilution Calculator

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Chemical Properties

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
Canonical SMILES CC1CCC(CC1)C(=O)N(C2CCC(CC2)O)C3=C(SC(=C3)C#CC(C)(C)C)C(=O)O
Formula C25H35NO4S M.Wt 445.6
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

Background

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.

Reference

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.