ProductDescription
VX-950(Telaprevir)isanorally-available,highly-selective,reversIBLe,peptidomimeticinhibitorofHCVNS3-4AproteasewithanIC50of0.35uMandIC90of0.83uMinanHCVrepliconassay[1,2]Inhumanfetalhepatocyteswithgenotype1aHCV-postivepatientserum,VX-950hasanIC50of280uM.[3]VX-950reducesHCVRNAlevelsinatime-anddose-dependentmannerwithIC50sof0.57,0.49,0.21,and0.14uMfollowinga24-,48-,72-,and120-hincubation.
VX-950formsacovalent,butreversiblecomplexinaslow-on,slow-ffprocesswithasteady-stateinhibitionconstant(Ki)of7nM.[3]ExcellentefficacywithhighliverexposureinanHCVNS3-4AmousemodelwasobservedwithVX-950.
Technicalinformation:
| ChemicalFormula: | C36H53N7O6 | |
| CAS#: | 402957-28-2 | |
| MolecularWeight: | 679.85 | |
| Purity: | >98% | |
| Appearance: | White | |
| ChemicalName: | (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: | Upto100mMinDMSO | |
| Synonyms: | VX-950,VX-950,Telaprevir,Incivek,Incivo |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
| 1. | Linetal.,VX-950,anovelhepatitisCvirus(HCV)NS3-4Aproteaseinhibitor,exhibitspotentantiviralactivitiesinHCvrepliconcells.Antimicrob.AgentsChemother.2006,50(5),1813-1822.PubmedID:16641454 |
| 2. | Linetal.,DiscoveryanddevelopmentofVX-950,anovel,covalent,andreversibleinhibitorofhepatitisCvirusNS3.4Aserineprotease.InfectiousDisorders:DrugTargets,2006,6(1),3-16.PubmedID:16787300 |
| 3. | Pernietal.,PreclinicalprofileofVX-950,apotent,selective,andorallybioavailableinhibitorofhepatitisCvirusNS3-4Aserineprotease.Antimicrob.AgentsChemother.2006,50(3),899-909.PubmedID:16495249 |
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