Telaprevir (VX-950)

Telaprevir (VX-950) is an HCV NS3-4A serine protease inhibitor with IC50 of 0.35 μM.

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Telaprevir (VX-950) Chemical Structure

Telaprevir (VX-950) Chemical Structure
Molecular Weight: 679.85

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Product Information

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Product Description

Biological Activity

Description Telaprevir (VX-950) is an HCV NS3-4A serine protease inhibitor with IC50 of 0.35 μM.
Targets HCV NS3-4A serine protease
IC50 0.35 μM [1]
In vitro Telaprevir inhibits the hepatitis C virus NS3-4A serine protease, leading to the block of viral polyprotein processing and subsequently decrease of viral RNA replication, total HCV RNA levels and protein levels in the Con1 (genotype 1b) subgenomic HCV replicon cells in a time- and dose-dependent manner. Telaprevir displays a significant time-dependent increase in inhibitory effect on the replication of HCV RNA with IC50 values of 0.574 μM, 0.488 μM, 0.210 μM and 0.139 μM for 24, 48, 72 and 120 hours incubation, respectively. Telaprevir displays an average IC50 of 0.354 μM and an average IC90 of 0.830 μM, respectively, from three independent experiments using the 48 hours incubation. Telaprevir has no significant cytotoxicity to HCV replicon cells, parental Huh-7 and HepG2 cells after 48 hours incubation. Telaprevir (17.5 μM) completely eradicates HCV RNA from replicon cells after 13 days incubation without rebound after Telaprevir is withdrawn. Telaprevir displays an additive to moderate synergistic effect on reduction of HCV RNA replication and suppression of resistance mutations without significant increase in cytotoxicity when in combination with IFN-α, compared to treatment with each agent alone. [1]
In vivo Oral administration of Telaprevir reduces HCV protease-dependent cleavage and subsequent secretion of SEAP from the liver into the blood in the mice model to 18.7% and 18.4% at dosage of 10 and 25 mg/kg, respectively. [2] Administration of Telaprevir at 200 mg/kg for 1 week results in a 1.9 log reduction of HCV RNA in genotype 1b HCV-infected human hepatocyte chimeric mice, and when treatment in combination with MK-0608 (50 mg/kg) for 4 weeks, viruses are eliminated from mice. [3]
Features Telaprevir is a covalent, reversible inhibitor of the NS3-4A protease (unlike BILN 2061which is a noncovalent inhibitor), with a slow-binding and slow-dissociation mechanism.

Protocol(Only for Reference)

Kinase Assay: [1]

Determination of anti-HCV activity Stable Huh-7 cells containing the self-replicating, subgenomic HCV replicon, which is identical in sequence to the I377neo/NS3-3'/wt replicon are used for anti-HCV assays. Replicon cells are incubated at 37 °C for the indicated period of time with Telaprevir serially diluted in DMEM plus 2% FBS and 0.5% dimethyl sulfoxide (DMSO). Total cellular RNA is extracted using an RNeasy-96 kit, and the copy number of HCV RNA is determined using a quantitative RTPCR (QRT-PCR) assay for the assessment of 50% inhibitory concentration (IC50

Cell Assay: [1]

Cell lines Huh-7, HepG2, and peripheral blood mononuclear cells (PBMC)
Concentrations Dissolved in DMSO, final concentration ~1 mM
Incubation Time 48 hours
Method Cells are incubated with various concentrations of Telaprevir for 48 hours. Cell viability is determined by using a tetrazolium (MTS)-based cell viability assay.

Animal Study: [2]

Animal Models SCID mice injected with recombinant adenovirus (Ad-WT-HCVpro-SEAP or Ad-MT-HCVpro-SEAP)
Formulation Formulated in polyvinylpyrrolidone (PVP) K-30 plus 2% sodium lauryl sulfate
Dosages ~300 mg/kg
Administration Oral gavage
Solubility 30% PEG400/0.5% Tween80/5% propylene glycol, , 30 mg/mL
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
1

References

[1] Lin K, et al. Antimicrob Agents Chemother, 2006, 50(5), 1813-1822.

[2] Perni RB, et al. Antimicrob Agents Chemother, 2006, 50(3), 899-909.

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Clinical Trial Information( data from http://clinicaltrials.gov)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT01994486 Recruiting Hepatitis C, Chronic University of Florida|Vertex Pharmaceuticals Incorporated 2013-12 Phase 2
NCT02006745 Recruiting HIV St Stephens Aids Trust 2014-01 Phase 3
NCT02124044 Recruiting HIV-HCV National Institutes of Health Clinical Center (CC)|National Institute of Allergy and Infectious Diseases (NIAID) 2014-02 Phase 2
NCT02087111 Not yet recruiting Hepatitis C Queen Mary University of London|Janssen-Cilag Ltd.|Barts & The London NHS Trust|St George's Healthcare NHS Trust|Bradford Teaching Hospitals NHS Foundation Trust|Nottingham University Hospitals NHS Trust 2014-04 Phase 4
NCT01945008 Recruiting Hepatitis C, Chronic Istituto Superiore di Sanita 2014-04

Chemical Information

Download Telaprevir (VX-950) SDF
Molecular Weight (MW) 679.85
Formula

C36H53N7O6

CAS No. 402957-28-2
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms LY-570310, MP-424
Solubility (25°C) * In vitro DMSO 136 mg/mL (200 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 30% PEG400/0.5% Tween80/5% propylene glycol, 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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

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Customer Reviews (1)


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Rating
Source Dr Julie Sheldon,Dr Esteban Domingo and Dr Celia Perales. Telaprevir (VX-950) purchased from Selleck
Method MTT assays
Cell Lines
Concentrations 50 μM
Incubation Time 72 h
Results The 50% cytotoxic concentration (CC50) of VX-950 was 22 ± 3.2 μM.

Product Citations (8)

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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