VX-222 is a small molecule non-nucleoside inhibitor of HCV NS5B polymerase that is being investigated for the treatment of hepatitis C virus infection. While the protease inhibitors (telaprevir and boceprevir) are the directly-targeted anti-HCV agents furthest along in the development pipeline, HCV polymerase - an enzyme responsible for copying viral genetic material-is also a promising target. VX-222 is a novel non-nucleoside HCV NS5B polymerase inhibitor with potent in vitro activity.
|Cell lines||Huh7.5 cells|
|Preparation method||Trypsinizing Huh7.5 cells harboring HCV RNA replicons and plating into 48-well plates at a concentration of 4 × 104 cells/well. Changing the medium and adding VX-222in 200 μL of complete medium the next day. 48 hours later, total RNA is extracted and viral RNAs are quantiﬁed by real-time reverse transcription-PCR (RT-PCR). The effective drug concentrations that reduced HCV RNA replicon levels by 50% (EC50) are calculated by nonlinear regression analysis with log curve ﬁtting|
|Concentrations||0.01 nM -10 μM|
|Incubation time||48 hours|
|Animal models||Rats or dogs|
|Formulation||Dissolved in 30% PEG|
|Dosages||5 mg/kg for rats or 10 mg/kg for dogs|
|Administration||By oral gavage|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 80 mg/mL|
|Related HCV Protease Products|
Ombitasvir is a potent inhibitor of the hepatitis C virus protein NS5A, with EC50s of 0.82 to 19.3 pM against HCV genotypes 1 to 5 and 366 pM against genotype 6a.
Paritaprevir (ABT-450) is a potent non-structural protein 3/4A (NS3/4A) protease inhibitor with EC50 values of 1 and 0.21 nM for HCV 1a and 1b, respectively.
Velpatasvir is a second-generation NS5A inhibitor that inhibits hepatitis C viral replication through acting on the crucial "membranous web" that facilitates RNA replication.
Lycorine hydrochloride is a natural alkaloid extracted from the Amaryllidaceae plant family, it is also an HCV inhibitor with strong activity.
Daclatasvir is a potent hepatitis C virus (HCV) NS5A protein inhibitor with picomolar EC50 value .
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