Tel: +1-832-582-8158

Product Categories

Telaprevir (VX-950)

Catalog No.S1538
1 Reviews 8 Product Citations

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

Price Stock Quantity  
USD 170 In stock
USD 270 In stock
USD 770 In stock
Contact Us
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

Selleck USA Tel: +1-832-582-8158[email protected]
Telaprevir (VX-950) Chemical Structure

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

Validation & Quality Control

Customer Reviews(1)

Quality Control & MSDS

Related Compound Libraries

Telaprevir (VX-950) is available in the following compound libraries:

Inhibitor Library Bioactive Compound Library

Product Information

  • Compare HCV Protease Inhibitors
    Compare HCV Protease Products
  • Research Area

Product Description

Biological Activity Protocol Clinical Trial Information Chemical Information Customer Reviews Product Citations Tech Support & FAQs

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μM) completely eradicates HCV RNA from replicon cells after 13 days incubation without rebound after Telaprevir is withdrawn.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.

view more

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
Molarity Calculator Dilution Calculator Molecular Weight Calculator

Research Area

Customer Reviews (1)


Click to enlarge 		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)

Customers Who Bought This Item Also Bought

  • Bortezomib (PS-341)

    Bortezomib (PS-341) is a potent 20S proteasome inhibitor with Ki of 0.6 nM.

  • Carfilzomib (PR-171)

    Carfilzomib (PR-171) is an irreversible proteasome inhibitor with IC50 of <5 nM, displayed preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, but little or no effect on the PGPH and T-L activities.

  • Raltegravir (MK-0518)

    Raltegravir (MK-0518) is a potent integrase (IN) inhibitor for WT and S217Q PFV IN with IC50 of 90 nM and 40 nM, respectively.

    Features:The 1st approved human immunodeficiency virus type 1 (HIV-1) integrase inhibitor.

  • Ibrutinib (PCI-32765)

    Ibrutinib is a potent and highly selective Btk inhibitor with IC50 of 0.5 nM, modestly potent to Bmx, CSK, FGR, BRK, HCK, less potent to EGFR, Yes, ErbB2, JAK3, etc.

  • Cilengitide

    Cilengitide is a potent integrin inhibitor for αvβ3 receptor and αvβ5 receptor with IC50 of 4.1 nM and 79 nM, respectively; ~10-fold selectivity against gpIIbIIIa. Phase 2.

  • Emtricitabine

    Emtricitabine is a nucleoside reverse transcriptase inhibitor with an IC50 of 27.7 μM.

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.

Handling Instructions
Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related HCV Protease Products

  • E-64

    E-64 is an irreversible and selective cysteine protease inhibitor with IC50 of 9 nM for papain.

  • NSC 405020

    NSC 405020 is a noncatalytic inhibitor of MT1-MMP, directly interacts with PEX domain of MT1-MMP, affects PEX homodimerization but not catalytic activity of MT1-MMP.

  • Aloxistatin

    Aloxistatin is an irreversible and membrane-permeable cysteine protease inhibitor.

  • Danoprevir (ITMN-191)

    Danoprevir(ITMN-191) is a peptidomimetic inhibitor of the NS3/4A protease of hepatitis C virus (HCV) with IC50 of 0.2-3.5 nM, inhibition effect for HCV genotypes 1A/1B/4/5/6 is ~10-fold higher than 2B/3A. Phase 2.

    Features:A peptidomimetic inhibitor of the NS3/4A protease of hepatitis C virus (HCV).

  • Daclatasvir (BMS-790052)

    BMS-790052 is a highly selective inhibitor of HCV NS5A with EC50 of 9-50 pM, for a broad range of HCV replicon genotypes and the JFH-1 genotype 2a infectious virus in cell culture. Phase 3.

    Features:First-in-class, highly selective inhibitor of hepatitis C virus (HCV) NS5A with picomolar EC50 values.

  • VX-222 (VCH-222, Lomibuvir)

    VX-222 (VCH-222) is a novel, potent and selective inhibitor of HCV polymerase with IC50 of 0.94-1.2 μM, 15.3-fold less effective for mutant M423T, and 108-fold less effective for mutant I482L. Phase 2.

    Features:A novel, potent and selective inhibitor of non-nucleoside polymerase, specifically the HCV RNA-dependent RNA polymerase.

  • MG-132

    MG-132 is an inhibitor of proteasome with IC50 of 100 nM, and also inhibits calpain with IC50 of 1.2 μM.

  • Bortezomib (PS-341)

    Bortezomib (PS-341) is a potent 20S proteasome inhibitor with Ki of 0.6 nM.

  • Carfilzomib (PR-171)

    Carfilzomib (PR-171) is an irreversible proteasome inhibitor with IC50 of <5 nM, displayed preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, but little or no effect on the PGPH and T-L activities.

  • ONX-0914 (PR-957)

    ONX-0914 (PR-957) is a potent and selective immunoproteasome inhibitor with minimal cross-reactivity for the constitutive proteasome.

    Features:The first highly selective, small molecule inhibitor of the immunoproteasome. Potential use in cancer and autoimmune diseases (e.g. rheumatoid arthritis, inflammatory bowel disease, and lupus).

Recently Viewed Items

Tags: buy Telaprevir (VX-950) | Telaprevir (VX-950) ic50 | Telaprevir (VX-950) price | Telaprevir (VX-950) cost | Telaprevir (VX-950) solubility dmso | Telaprevir (VX-950) purchase | Telaprevir (VX-950) manufacturer | Telaprevir (VX-950) research buy | Telaprevir (VX-950) order | Telaprevir (VX-950) mouse | Telaprevir (VX-950) chemical structure | Telaprevir (VX-950) mw | Telaprevir (VX-950) molecular weight | Telaprevir (VX-950) datasheet | Telaprevir (VX-950) supplier | Telaprevir (VX-950) in vitro | Telaprevir (VX-950) cell line | Telaprevir (VX-950) concentration | Telaprevir (VX-950) nmr
Contact Us