VX-950 (Telaprevir) is an orally-available, highly-selective, reversible, peptidomimetic inhibitor of HCV NS3-4A protease with an IC50 of 0.35 uM and IC90 of 0.83 uM in an HCV replicon assay [1, 2] In human fetal hepatocytes with genotype 1a HCV-postive patient serum, VX-950 has an IC50 of 280 uM. [3] VX-950 reduces HCV RNA levels in a time- and dose-dependent manner with IC50s of 0.57, 0.49, 0.21, and 0.14 uM following a 24-, 48-, 72-, and 120-h incubation.
VX-950 forms a covalent, but reversible complex in a slow-on, slow-ff process with a steady-state inhibition constant (Ki) of 7 nM. [3] Excellent efficacy with high liver exposure in an HCV NS3-4A mouse model was observed with VX-950.
Technical information:
| Chemical Formula: | C36H53N7O6 | |
| CAS #: | 402957-28-2 | |
| Molecular Weight: | 679.85 | |
| Purity: | >98% | |
| Appearance: | White | |
| Chemical Name: | (1S,3aR,6aS)-2-((S)-2-((S)-2-cyclohexyl-2-(pyrazine-2-carboxamido)acetamido)-3,3-dimethylbutanoyl)-N-((S)-1-(cyclopropylamino)-1,2-dioxohexan-3-yl)-octahydrocyclopenta[c]pyrrole-1-carboxamide | |
| Solubility: | Up to 100mM in DMSO | |
| Synonyms: | VX-950, VX-950, Telaprevir, Incivek, Incivo |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Lin et al., VX-950, a novel hepatitis C virus (HCV) NS3-4A protease inhibitor, exhibits potent antiviral activities in HCv replicon cells. Antimicrob. Agents Chemother. 2006, 50(5), 1813-1822. Pubmed ID: 16641454 |
| 2. | Lin et al., Discovery and development of VX-950, a novel, covalent, and reversible inhibitor of hepatitis C virus NS3.4A serine protease. Infectious Disorders: Drug Targets, 2006, 6(1), 3-16. Pubmed ID: 16787300 |
| 3. | Perni et al., Preclinical profile of VX-950, a potent, selective, and orally bioavailable inhibitor of hepatitis C virus NS3-4A serine protease. Antimicrob. Agents Chemother. 2006, 50(3), 899-909. Pubmed ID: 16495249 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
