Telaprevir (VX-950)

Catalog No.S1538 Synonyms: LY-570310, MP-424

Telaprevir (VX-950) Chemical Structure

Molecular Weight(MW): 679.85

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

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4 Customer Reviews

  • HCV replicon genotype 1b cells were passaged in the presence of G418 alone (medium 694 control) or G418 with miravirsen, SPC4729 (oligonucleotide negative control) or telaprevir for 28 days in fixed concentrations at a multiple (X) of the EC50 of miravirsen or telaprevir. Colony formation was assessed by staining surviving cells with crystal violet.

    Antimicrob Agents Chemother 2014 10.1128/AAC.04220-14. Telaprevir (VX-950) purchased from Selleck.

    Cleavage of DDB1 by NS3/4A is inhibited by the NS3/4A inhibitor VX-950. The 293 cells were transfected with N-terminal or C-terminal Flag-tagged DDB1 (N-Flag-DDB1 or DDB1-C-Flag respectively) and HA-NS3/4A. The transfected cells were treated with VX-950 (0.2 mM) or left untreated for 1 day before immunoblot analysis with anti-Flag or anti-HA.

    Virology 2013 435(2), 385-94. Telaprevir (VX-950) purchased from Selleck.

  • VX950, a HCV NS3/4A protease inhibitor, abrogates cleavage of C4 induced by HCV NS3/4A protease. VX950 was added to HCV NS3/4A protease at the indicated concentrations, and then C4 was added. Proteins were separated by SDS-PAGE for CBB staining. The three C4-derived fragments of 17 kDa and 15 kDa produced by NS3/4A protease action could not be detected after pretreatment with VX950, and this change was accompanied by an increased concentration of the 32-kDa C4γchain.

    PLoS One 2013 8(12), e82094. Telaprevir (VX-950) purchased from Selleck.

    The toxicity of BMS-790052 (BMS) and Telaprevir (TPV) was measured by seeding 96-well plates to 70% confluence and exposing the cells to up to 50 μM of compound for 72 hours. MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] was added to each well at a final concentration of 500 μg/ml 4 h before dissolving crystals in 100 μl of DMSO and measuring at 550 nm UV wavelengths. The 50% cytotoxic concentration (CC50) was then calculation using the OD550 value and the following formula: log CC50=log concentration of HPP-[(HPP-50)/(HPP-LPP)×log d HPP: highest protective percentage closest to 50% LPP: Lowest protective percentage closest to 50% d: dilution factor

    2011 Dr. Julie Sheldon,Dr Esteban Domingo and Dr Celia Perales. Telaprevir (VX-950) purchased from Selleck.

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Biological Activity

Description Telaprevir (VX-950) is an HCV NS3-4A serine protease inhibitor with IC50 of 0.35 μM.
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.
Targets
HCV NS3-4A serine protease [1]
0.35 μM
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]

Protocol

Kinase Assay:[1]
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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 Research:[1]
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  • 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.
    (Only for Reference)
Animal Research:[2]
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  • 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
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 136 mg/mL (200.04 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
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 Information

Molecular Weight 679.85
Formula

C36H53N7O6

CAS No. 402957-28-2
Storage powder
in solvent
Synonyms LY-570310, MP-424

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02333292 Recruiting Chronic Hepatitis C Infection Valme University Hospital|Hospital del SAS de Jerez|Hospital General Universitario Elche|Hospital La Línea de la Concepción|Complexo Hospitalario Universitario de A Coruña|Hospital de Figueres|Hospital Universitario Puerto Real|Hospital Universitario Virgen de la Victoria|Hospital Universitario de Canarias|Hospital General Universitario de Alicante|Hospital Universitario Araba|Hospital Royo Vilanova|Hospital Universitario de Burgos|Complejo Hospitalario Universitario de Huelva|Hospital Universitario Reina Sofia|Hospital Universitario Virgen Macarena|Complexo Hospitalario Universitario de Vigo|Clinica Universidad de Navarra, Universidad de Navarra|Hospital Clinico Universitario San Cecilio|Hospital Universitario La Fe|Hospital General Universitario de Valencia|Hospital Universitario Infanta Leonor|Hospital Universitario de Gran Canaria|Hospital General Universitario Santa Lucía|Centro Penitenciario Alicante 1|Hospital Regional Universitario Carlos Haya|Hospital Virgen de la Luz|Hospital General Universitario de Castellón|Hospital Parc Taulí, Sabadell December 2014 --
NCT02087111 Unknown status Hepatitis C Queen Mary University of London|Janssen-Cilag Ltd.|Barts & The London NHS Trust|St Georges Healthcare NHS Trust|Bradford Teaching Hospitals NHS Foundation Trust|Nottingham University Hospitals NHS Trust April 2014 Phase 4
NCT02006745 Completed HIV St Stephens Aids Trust January 2014 Phase 3
NCT01994486 Completed Hepatitis C, Chronic University of Florida|Vertex Pharmaceuticals Incorporated December 2013 Phase 2
NCT01890772 Withdrawn Hepatitis C Timothy Morgan, MD|Vertex Pharmaceuticals Incorporated|Southern California Institute for Research and Education August 2013 Phase 2|Phase 3
NCT01872936 Unknown status Hepatitis C, Chronic Santaris Pharma A/S June 2013 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID