Telaprevir (VX-950)

For research use only.

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

28 publications

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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Selleck's Telaprevir (VX-950) has been cited by 28 publications

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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μM) completely eradicates HCV RNA from replicon cells after 13 days incubation without rebound after Telaprevir is withdrawn.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)
  • Dosages: ~300 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 136 mg/mL (200.04 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.
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.

Chemical Information

Molecular Weight 679.85
Formula

C36H53N7O6

CAS No. 402957-28-2
Storage powder
in solvent
Synonyms LY-570310, MP-424
Smiles CCCC(NC(=O)C1C2CCCC2CN1C(=O)C(NC(=O)C(NC(=O)C3=NC=CN=C3)C4CCCCC4)C(C)(C)C)C(=O)C(=O)NC5CC5

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02881034 Completed Drug: Triple therapy Hepatitis C Hospices Civils de Lyon February 2014 --
NCT01994486 Completed Drug: Telaprevir and Sofosbuvir Hepatitis C Chronic University of Florida|Vertex Pharmaceuticals Incorporated December 2013 Phase 2
NCT01980290 Completed -- Hepatitis Chronic Janssen Pharmaceutica N.V. Belgium May 2013 --
NCT01841502 Terminated Drug: Paroxetine|Drug: telaprevir Hepatitis C Infection|Depression Radboud University|Janssen LP May 2013 Phase 2
NCT01766167 Completed Drug: MP-424 Chronic Hepatitis C Mitsubishi Tanabe Pharma Corporation February 2013 Phase 1

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID