1. Anti-infection Metabolic Enzyme/Protease
  2. HCV Protease HCV SARS-CoV
  3. Telaprevir

Telaprevir (VX-950) is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide. Telaprevir inhibits SARS-CoV-2 3CLpro activity.

For research use only. We do not sell to patients.

Telaprevir Chemical Structure

Telaprevir Chemical Structure

CAS No. : 402957-28-2

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Customer Review

Based on 50 publication(s) in Google Scholar

Other Forms of Telaprevir:

Top Publications Citing Use of Products

43 Publications Citing Use of MCE Telaprevir

WB
Proliferation Assay

    Telaprevir purchased from MedChemExpress. Usage Cited in: Eur J Med Chem. 2018 Jan 1;143:1053-1065.  [Abstract]

    GS4.3 cells are treated with 7f (20 μM), or Telaprevir (0.5μM), GS-7977 (0.8 μM), BMS-790052 (0.15 μM) or solvent control for 6 days.

    Telaprevir purchased from MedChemExpress. Usage Cited in: Biomed Res Int. 2017;2017:1236801.  [Abstract]

    Naïve Huh7.5 cells are infected with wild and mutant type HCV and simultaneously treated with drugs. Intracellular proteins were extracted and detected with WB in 72 hours. Telaprevir (VX-950) against WT and A156T mutant HCV.

    Telaprevir purchased from MedChemExpress. Usage Cited in: Sci Rep. 2016 Feb 22;6:21808.  [Abstract]

    While compounds SSO and VX-950 show HCV inhibitory activity in the Group 1 (P < 0.01), SSO-treated viruses display infectivity equal to that of untreated control and negative reference VX-950 in Group 2 (P > 0.05).

    Telaprevir purchased from MedChemExpress. Usage Cited in: Antiviral Res. 2015 Dec;124:54-60.  [Abstract]

    Cell lysates at 52 h.p.e are analysed by western blot for NS5A and GAPDH. Both 160 and Telaprevir cause a comparable reduction in NS5A relative to DMSO control.

    Telaprevir purchased from MedChemExpress. Usage Cited in: Antimicrob Agents Chemother. 2015 Dec;59(12):7666-7670.  [Abstract]

    Effects of antiviral drugs on cellular uptake of Resorcinol phthalein by BeWo cells. The cells are incubated with 1 μM Resorcinol phthalein in the presence of 100 μM compounds for 10 min at 37°C.

    Telaprevir purchased from MedChemExpress. Usage Cited in: Virology. 2014 May;456-457:300-9.  [Abstract]

    Jurkat cells are transfected with plasmids expressing (A) HCV NS3/4A or (B) HPgV NS3/4AB-HA. Telaprevir, EBP 520, and Danoprevir are added at concentrations of 100 µM, 16.6 µM, 2.7 µM, or 0 µM in 0.1% DMSO. Lysates are harvested after 24 h and resolved by immunoblots probed with anti-HCV NS3 (A) or anti-HA (B). The position of HCV NS3/4A (~75kDa), HCV NS3 (~73kDa), NS3/4AB-HA, and NS4B-HA (~30kDa) are indicated. Molecular markers are on the right.

    Telaprevir purchased from MedChemExpress. Usage Cited in: Open Virol J. 2014 Mar 7;8:1-8.  [Abstract]

    The PKR activation block is not unique to CypI, DAAs also prevent the IFN-induced PKR activation in HCV-infected cells. JFH-1-infected Huh7.5.1 cells are treated with or without CypI (CsA and alisporivir), DAAs (the HCV NS5A inhibitor BMS-790052 and the HCV protease inhibitor telaprevir) and an HIV-1 inhibitor (reverse transcriptase inhibitor BW1592). Results are representative of 4 independent experiments.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Telaprevir (VX-950) is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide[1][2][3]. Telaprevir inhibits SARS-CoV-2 3CLpro activity[4].

    IC50 & Target

    Ki: 7 nM (genotype 1 HCV NS3-4A protease)[1]

    In Vitro

    Telaprevir (VX-950) is a covalent, reversible inhibitor of the NS3-4A protease with a slow-binding and slow-dissociation mechanism. Telaprevir exhibits significantly different kinetics in enzyme inhibition, which is most clearly exemplified by a very long half-life (58 min) of the bound enzyme-inhibitor complex. Telaprevir is additive to moderately synergistic with IFN-α in inhibiting HCV replication and in suppressing the emergence of resistance in replicon cells. Telaprevir reduces HCV RNA levels in a time- and dose-dependent manner. The IC50s following a 24, 48, 72, and 120 h incubation with Telaprevir are determined to be 0.574, 0.488, 0.21, and 0.139 μM, respectively, indicating an increase in inhibitory effects with time. Following three independent experiments using the 48 h incubation in the presence of 2% FBS, the average IC50 of Telaprevir is determined to be 0.354 ± 0.035 μM, and the average IC90 is 0.830 ± 0.190 μM[1]. Telaprevir (VX-950) is a potent, selective, peptidomimetic inhibitor of the hepatitis C virus (HCV) NS3-4A serine protease, and Telaprevir demonstrates excellent antiviral activity both in genotype 1b HCV replicon cells (IC50=354 nM) and in human fetal hepatocytes infected with genotype 1a HCV-positive patient sera (IC50=280 nM)[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    There is an ~5-fold reduction of serum SEAP activity in mice dosed with Telaprevir (VX-950) at either 10 or 25 mg/kg, which has an average value (±SEM) of 18.7±8.3% or 18.4±5.4%, respectively, compare to those administered vehicle (100±28%). These data demonstrates that Telaprevir is able to inhibit the HCV NS3-4A serine protease activity in mouse liver and block cleavage and subsequent secretion of SEAP into blood circulation in these mice[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    Molecular Weight

    679.85

    Formula

    C36H53N7O6

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(N([C@@H]1C(N[C@H](C(C(NC2CC2)=O)=O)CCC)=O)C[C@@]3(CCC[C@@]31[H])[H])[C@@H](NC([C@@H](NC(C4=NC=CN=C4)=O)C5CCCCC5)=O)C(C)(C)C

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 50 mg/mL (73.55 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.4709 mL 7.3546 mL 14.7091 mL
    5 mM 0.2942 mL 1.4709 mL 2.9418 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (3.68 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.54%

    References
    Cell Assay
    [1]

    Determination of IC50, IC90, CC50 of Telaprevir (VX-950) or IFN-α in HCV replicon cells is performed. Briefly, 1×104 replicon cells per well are plated in 96-well plates. On the following day, replicon cells is incubated at 37°C for the indicated period of time with antiviral agents serially diluted in DMEM plus 2% FBS and 0.5% DMSO. Total cellular RNA is extracted using an RNeasy-96 kit, and the copy number of HCV RNA is determined using a quantitative RT-PCR (QRT-PCR) assay. Each datum point represents the average of five replicates in cell culture. The cytotoxicity of Telaprevir is measured under the same experimental settings using a tetrazolium (MTS)-based cell viability assay. For the cytotoxicity assay with human hepatocyte cell lines, 1×104 parental Huh-7 cells per well or 4×104 HepG2 cells per well are used. To determine cytotoxicity of Telaprevir against resting PBMC, 1×105 cells per well are incubated with Telaprevir in RPMI-1640 medium (no serum) for 48 h, and the cell viability is determined by the MTS-based assay. To determine cytotoxicity of VX-950 against proliferating PBMC, 1×105 cells per well in RPMI-1640 medium are added to a 96-well plate, which is precoated with anti-human CD3 antibody. The cells are incubated with Telaprevir and anti-human CD28 antibody for 72 h at 37°C, and the cell growth is determined by [3H]thymidine update between the 48th and 72nd h[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2]

    Mice[2]
    Five groups of 6-week-old SCID mice (6 animals per group) are injected with 109 IFU per mouse of recombinant adenovirus Ad-WT-HCVpro-SEAP through the tail vein. Each group of mice is given two oral administrations of Telaprevir (VX-950) at one of the following doses: 10, 25, 75, 150, or 300 mg/kg. The first Telaprevir dose is given 2 h before the adenovirus injection, and the second dose is given 10 h after injection. An additional group of 10 mice is given vehicle alone. Serum samples are collected 24 h postinjection, and the SEAP activity in each Telaprevir-dosed group is compared to that of the vehicle group. Rat and Dog[2] The intravenous and oral pharmacokinetics of Telaprevir (VX-950) are evaluated in rats and dogs. A group of 3 male Sprague-Dawley rats weighing 250 to 300 g is administered an intravenous bolus dose of 0.95 mg/kg Telaprevir. Serial blood samples are collected in heparinized tubes before dosing and at 0.083, 0.167, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, and 8 h after dose administration. A group of 3 male beagle dogs (8 to 12 kg) is administered an intravenous bolus dose of 3.5 mg/kg Telaprevir in 10% ethanol, 40% polyethylene glycol 400, and 50% D5W. Serial blood samples are collected in heparinized tubes before dosing and at 0.083, 0.167, 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12, and 24 h after dose administration. For oral studies in rats and dogs, Telaprevir is formulated in polyvinylpyrrolidone (PVP) K-30 plus 2% sodium lauryl sulfate and then dosed as an oral gavage. A group of 3 male Sprague-Dawley rats (250 to 300 g) is dosed orally with 40 mg/kg VX-950, and a group of 4 male beagle dogs (10.9 to 12.0 kg) is administered an oral dose of 9.6 mg/kg VX-950. In both oral studies, blood samples are taken before dosing and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, and 24 h after dose administration. In both intravenous and oral studies, plasma samples are obtained by centrifugation and stored at −70°C until analysis. Samples from the intravenous studies are analyzed by a chiral liquid chromatography followed by tandem mass spectrometry (LC/MS/MS) method, and samples from the oral studies are analyzed using an achiral LC/MS/MS method.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.4709 mL 7.3546 mL 14.7091 mL 36.7728 mL
    5 mM 0.2942 mL 1.4709 mL 2.9418 mL 7.3546 mL
    10 mM 0.1471 mL 0.7355 mL 1.4709 mL 3.6773 mL
    15 mM 0.0981 mL 0.4903 mL 0.9806 mL 2.4515 mL
    20 mM 0.0735 mL 0.3677 mL 0.7355 mL 1.8386 mL
    25 mM 0.0588 mL 0.2942 mL 0.5884 mL 1.4709 mL
    30 mM 0.0490 mL 0.2452 mL 0.4903 mL 1.2258 mL
    40 mM 0.0368 mL 0.1839 mL 0.3677 mL 0.9193 mL
    50 mM 0.0294 mL 0.1471 mL 0.2942 mL 0.7355 mL
    60 mM 0.0245 mL 0.1226 mL 0.2452 mL 0.6129 mL
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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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