Home Proteases HCV Protease inhibitor - COVID-19 inhibitor Telaprevir For research use only.

Telaprevir

Synonyms: LY-570310, MP-424,VX-950

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

Telaprevir Chemical Structure

Telaprevir Chemical Structure

CAS No. 402957-28-2

Purity & Quality Control

Telaprevir Related Products

Signaling Pathway

HCV Protease Signaling Pathways

HCV Protease Signaling Pathway

Biological Activity

Description Telaprevir 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
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μM) completely eradicates HCV RNA from replicon cells after 13 days incubation without rebound after Telaprevir is withdrawn.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]
Kinase Assay 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 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.
In Vivo
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]
Animal Research Animal Models SCID mice injected with recombinant adenovirus (Ad-WT-HCVpro-SEAP or Ad-MT-HCVpro-SEAP)
Dosages ~300 mg/kg
Administration Oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02881034 Completed
Hepatitis C
Hospices Civils de Lyon
 February 2014 --
NCT01994486 Completed
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
Hepatitis C Infection|Depression
Radboud University Medical Center|Janssen LP
 May 2013 Phase 2
NCT01766167 Completed
Chronic Hepatitis C
Mitsubishi Tanabe Pharma Corporation
 February 2013 Phase 1

Chemical Information & Solubility

Molecular Weight 679.85 Formula

C36H53N7O6
CAS No. 402957-28-2 SDF Download Telaprevir SDF
Smiles CCCC(C(=O)C(=O)NC1CC1)NC(=O)C2C3CCCC3CN2C(=O)C(C(C)(C)C)NC(=O)C(C4CCCCC4)NC(=O)C5=NC=CN=C5
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 136 mg/mL ( (200.04 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

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

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