Cat. No.: HY-10235

Telaprevir

(Synonyms: VX-950)

44 Cited Publications

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Based on 44 publication(s) in Google Scholar

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

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Purity: 99.77%
CAS No.: 402957-28-2
Formula: C₃₆H₅₃N₇O₆
Molecular Weight:679.85

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Telaprevir Chemical Structure

CAS No.: 402957-28-2

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (44)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
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Bioz

Biological Activity

Description

IC₅₀ & Target

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

Cellular Effect

Cell Line	Type	Value	Description	References
Hepatocyte	CC₅₀	90 μM Compound: VR-950	Cytotoxicity against human hepatocytes by MTT assay Cytotoxicity against human hepatocytes by MTT assay	[PMID: 19345581]
Huh-5-2	CC₅₀	>33 μM Compound: VX-950	Cytotoxicity against human Huh5-2 cells after 3 days by MTT assay Cytotoxicity against human Huh5-2 cells after 3 days by MTT assay	[PMID: 18625766]
Huh-5-2	EC₅₀	1 μM Compound: VX-950	Antiviral activity against Hepatitis C virus genotype 1b infected in human Huh5-2 cells assessed as reduction in replicon RNA after 4 days by luciferase assay Antiviral activity against Hepatitis C virus genotype 1b infected in human Huh5-2 cells assessed as reduction in replicon RNA after 4 days by luciferase assay	[PMID: 18625766]
Huh-5-2	CC₅₀	47 μM Compound: VX-950	Cytotoxicity against human Huh5-2 cells after 72 hrs by MTS assay Cytotoxicity against human Huh5-2 cells after 72 hrs by MTS assay	[PMID: 25617695]
Huh-5-2	CC₅₀	47 μM Compound: VX-950	Cytotoxicity against human HuH5.2 cells assessed as reduction in metabolic activity after 72 hrs by MTS assay Cytotoxicity against human HuH5.2 cells assessed as reduction in metabolic activity after 72 hrs by MTS assay	[PMID: 27474921]
Huh-5-2	CC₅₀	47 μM Compound: VX-950	Cytotoxicity against human HuH5.2 cells assessed as reduction in cell viability after 72 hrs by MTS assay Cytotoxicity against human HuH5.2 cells assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 27810598]
Huh-5-2	CC₅₀	>74 μM Compound: Telaprevir	Cytostatic activity against human Huh5-2 cells assessed as decrease in cell proliferation after 3 days by MTS method Cytostatic activity against human Huh5-2 cells assessed as decrease in cell proliferation after 3 days by MTS method	10.1039/C1MD00227A
Huh-5-2	EC₅₀	235 nM Compound: Telaprevir	Antiviral activity against Hepatitis C virus genotype 1b I389luc-ubi-neo/NS3-3'/5.1 subgenomic replicon infected in human Huh5-2 cells after 4 days by luciferase assay Antiviral activity against Hepatitis C virus genotype 1b I389luc-ubi-neo/NS3-3'/5.1 subgenomic replicon infected in human Huh5-2 cells after 4 days by luciferase assay	10.1039/C1MD00227A
Huh-7	CC₅₀	82 μM Compound: 1, Telaprevir	Cytotoxicity against Huh7 cells by MTS assay Cytotoxicity against Huh7 cells by MTS assay	[PMID: 17482818]
Huh-7	IC₅₀	0.49 μM Compound: telaprevir, (VX-950)	Antiviral activity against wild type HCV 1b Con1 in human Huh7 cells after 48 hrs by replicon cell assay Antiviral activity against wild type HCV 1b Con1 in human Huh7 cells after 48 hrs by replicon cell assay	[PMID: 17556358]
Huh-7	IC₅₀	11.7 μM Compound: telaprevir, (VX-950)	Antiviral activity against HCV 1b with NS3-4A R155I mutation in human Huh7 cells after 48 hrs by replicon cell assay Antiviral activity against HCV 1b with NS3-4A R155I mutation in human Huh7 cells after 48 hrs by replicon cell assay	[PMID: 17556358]
Huh-7	IC₅₀	2.7 μM Compound: telaprevir, (VX-950)	Antiviral activity against HCV 1b with NS3-4A R155M mutation in human Huh7 cells after 48 hrs by replicon cell assay Antiviral activity against HCV 1b with NS3-4A R155M mutation in human Huh7 cells after 48 hrs by replicon cell assay	[PMID: 17556358]
Huh-7	IC₅₀	3.6 μM Compound: telaprevir, (VX-950)	Antiviral activity against HCV 1b Con1 with NS3-4A R155K mutation in human Huh7 cells after 48 hrs by replicon cell assay Antiviral activity against HCV 1b Con1 with NS3-4A R155K mutation in human Huh7 cells after 48 hrs by replicon cell assay	[PMID: 17556358]
Huh-7	IC₅₀	3.6 μM Compound: telaprevir, (VX-950)	Antiviral activity against HCV 1b with NS3-4A R155G mutation in human Huh7 cells after 48 hrs by replicon cell assay Antiviral activity against HCV 1b with NS3-4A R155G mutation in human Huh7 cells after 48 hrs by replicon cell assay	[PMID: 17556358]
Huh-7	EC₅₀	>30 μM Compound: VX-950	Antiviral activity against HCV Con1-mADE replicon with NS3 serine protease V36A/R155T double mutation in human HuH7 cells after 48 hrs by RNA replicon assay Antiviral activity against HCV Con1-mADE replicon with NS3 serine protease V36A/R155T double mutation in human HuH7 cells after 48 hrs by RNA replicon assay	[PMID: 17938182]
Huh-7	EC₅₀	>30 μM Compound: VX-950	Antiviral activity against HCV Con1-mADE replicon with NS3 serine protease V36M/A156T double mutation in human HuH7 cells after 48 hrs by RNA replicon assay Antiviral activity against HCV Con1-mADE replicon with NS3 serine protease V36M/A156T double mutation in human HuH7 cells after 48 hrs by RNA replicon assay	[PMID: 17938182]
Huh-7	EC₅₀	>30 μM Compound: VX-950	Antiviral activity against HCV Con1-mADE replicon with NS3 serine protease V36M/R155T double mutation in human HuH7 cells after 48 hrs by RNA replicon assay Antiviral activity against HCV Con1-mADE replicon with NS3 serine protease V36M/R155T double mutation in human HuH7 cells after 48 hrs by RNA replicon assay	[PMID: 17938182]
Huh-7	EC₅₀	0.49 μM Compound: VX-950	Antiviral activity against wild type Con1-mADE HCV replicon in human HuH7 cells after 48 hrs by RNA replicon assay Antiviral activity against wild type Con1-mADE HCV replicon in human HuH7 cells after 48 hrs by RNA replicon assay	[PMID: 17938182]
Huh-7	EC₅₀	1.1 μM Compound: VX-950	Antiviral activity against HCV Con1-mADE replicon with NS3 serine protease V36L mutation in human HuH7 cells after 48 hrs by RNA replicon assay Antiviral activity against HCV Con1-mADE replicon with NS3 serine protease V36L mutation in human HuH7 cells after 48 hrs by RNA replicon assay	[PMID: 17938182]
Huh-7	EC₅₀	20 μM Compound: VX-950	Antiviral activity against HCV Con1-mADE replicon with NS3 serine protease V36A/R155K double mutation in human HuH7 cells after 48 hrs by RNA replicon assay Antiviral activity against HCV Con1-mADE replicon with NS3 serine protease V36A/R155K double mutation in human HuH7 cells after 48 hrs by RNA replicon assay	[PMID: 17938182]
Huh-7	EC₅₀	3 μM Compound: VX-950	Antiviral activity against HCV Con1-mADE replicon with NS3 serine protease T54A double mutation in human HuH7 cells after 48 hrs by RNA replicon assay Antiviral activity against HCV Con1-mADE replicon with NS3 serine protease T54A double mutation in human HuH7 cells after 48 hrs by RNA replicon assay	[PMID: 17938182]
Huh-7	EC₅₀	3.4 μM Compound: VX-950	Antiviral activity against HCV Con1-mADE replicon with NS3 serine protease V36M mutation in human HuH7 cells after 48 hrs by RNA replicon assay Antiviral activity against HCV Con1-mADE replicon with NS3 serine protease V36M mutation in human HuH7 cells after 48 hrs by RNA replicon assay	[PMID: 17938182]
Huh-7	EC₅₀	3.6 μM Compound: VX-950	Antiviral activity against HCV Con1-mADE replicon with NS3 serine protease V36A mutation in human HuH7 cells after 48 hrs by RNA replicon assay Antiviral activity against HCV Con1-mADE replicon with NS3 serine protease V36A mutation in human HuH7 cells after 48 hrs by RNA replicon assay	[PMID: 17938182]
Huh-7	EC₅₀	30 μM Compound: VX-950	Antiviral activity against HCV Con1-mADE replicon with NS3 serine protease V36M/R155K double mutation in human HuH7 cells after 48 hrs by RNA replicon assay Antiviral activity against HCV Con1-mADE replicon with NS3 serine protease V36M/R155K double mutation in human HuH7 cells after 48 hrs by RNA replicon assay	[PMID: 17938182]
Huh-7	EC₅₀	5.4 μM Compound: VX-950	Antiviral activity against HCV Con1-mADE replicon with NS3 serine protease V36G mutation in human HuH7 cells after 48 hrs by RNA replicon assay Antiviral activity against HCV Con1-mADE replicon with NS3 serine protease V36G mutation in human HuH7 cells after 48 hrs by RNA replicon assay	[PMID: 17938182]
Huh-7	EC₅₀	9.4 μM Compound: VX-950	Antiviral activity against HCV Con1-mADE replicon with NS3 serine protease V36A/T54A double mutation in human HuH7 cells after 48 hrs by RNA replicon assay Antiviral activity against HCV Con1-mADE replicon with NS3 serine protease V36A/T54A double mutation in human HuH7 cells after 48 hrs by RNA replicon assay	[PMID: 17938182]
Huh-7	EC₅₀	320 nM Compound: VX-950	Antiviral activity against wild-type Hepatitis C virus genotype 1b N infected in human Huh7 cells Antiviral activity against wild-type Hepatitis C virus genotype 1b N infected in human Huh7 cells	[PMID: 18086851]
Huh-7	CC₅₀	26.7 μM Compound: VX-950	Cytotoxicity against human HuH7 cells Cytotoxicity against human HuH7 cells	[PMID: 18285474]
Huh-7	EC₅₀	0.56 μM Compound: VX-950	Antiviral activity against Hepatitis C virus subtype 1b Con1 infected in human HuH7 cells after 3 days by luciferase reporter gene assay Antiviral activity against Hepatitis C virus subtype 1b Con1 infected in human HuH7 cells after 3 days by luciferase reporter gene assay	[PMID: 18285474]
Huh-7	CC₅₀	>50 μM Compound: 1, VX-950	Cytotoxicity against human HuH7 cells Cytotoxicity against human HuH7 cells	[PMID: 19285390]
Huh-7	EC₅₀	1600 nM Compound: 1, VX-950	Antiviral activity against HCV replication infected in human HuH7 cells after 96 hrs by replicon assay in presence of 10% FCS Antiviral activity against HCV replication infected in human HuH7 cells after 96 hrs by replicon assay in presence of 10% FCS	[PMID: 19285390]
Huh-7	EC₅₀	354 nM Compound: 1, VX-950	Antiviral activity against HCV replication infected in human HuH7 cells after 48 hrs by replicon assay in presence of 2% FCS Antiviral activity against HCV replication infected in human HuH7 cells after 48 hrs by replicon assay in presence of 2% FCS	[PMID: 19285390]
Huh-7	EC₅₀	102 nM Compound: Telaprevir	Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168H mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168H mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay	[PMID: 20176898]
Huh-7	EC₅₀	113 nM Compound: Telaprevir	Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168E mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168E mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay	[PMID: 20176898]
Huh-7	EC₅₀	147 nM Compound: Telaprevir	Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168N mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168N mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay	[PMID: 20176898]
Huh-7	EC₅₀	147 nM Compound: Telaprevir	Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80K mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80K mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay	[PMID: 20176898]
Huh-7	EC₅₀	1470 nM Compound: Telaprevir	Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 R155K mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 R155K mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay	[PMID: 20176898]
Huh-7	EC₅₀	150 nM Compound: Telaprevir	Antiviral activity against Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay Antiviral activity against Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay	[PMID: 20176898]
Huh-7	EC₅₀	15470 nM Compound: Telaprevir	Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 A156V mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 A156V mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay	[PMID: 20176898]
Huh-7	EC₅₀	1565 nM Compound: Telaprevir	Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 T54A mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 T54A mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay	[PMID: 20176898]
Huh-7	EC₅₀	181 nM Compound: Telaprevir	Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168T mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168T mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay	[PMID: 20176898]
Huh-7	EC₅₀	187 nM Compound: Telaprevir	Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168Y mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168Y mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay	[PMID: 20176898]
Huh-7	EC₅₀	202 nM Compound: Telaprevir	Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80G mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80G mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay	[PMID: 20176898]
Huh-7	EC₅₀	20326 nM Compound: Telaprevir	Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 A156T mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 A156T mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay	[PMID: 20176898]
Huh-7	EC₅₀	216 nM Compound: Telaprevir	Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80R mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80R mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay	[PMID: 20176898]
Huh-7	EC₅₀	22663 nM Compound: Telaprevir	Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 R155T mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 R155T mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay	[PMID: 20176898]
Huh-7	EC₅₀	2957 nM Compound: Telaprevir	Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80K and R155K mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80K and R155K mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay	[PMID: 20176898]
Huh-7	EC₅₀	300 nM Compound: Telaprevir	Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 V36L mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 V36L mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay	[PMID: 20176898]
Huh-7	EC₅₀	3107 nM Compound: Telaprevir	Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 A156S mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 A156S mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay	[PMID: 20176898]
Huh-7	EC₅₀	4106 nM Compound: Telaprevir	Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 R155M mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 R155M mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay	[PMID: 20176898]
Huh-7	EC₅₀	46 nM Compound: Telaprevir	Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168A mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168A mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay	[PMID: 20176898]
Huh-7	EC₅₀	570 nM Compound: Telaprevir	Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 R155Q mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 R155Q mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay	[PMID: 20176898]
Huh-7	EC₅₀	58 nM Compound: Telaprevir	Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 A156G mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 A156G mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay	[PMID: 20176898]
Huh-7	EC₅₀	66 nM Compound: Telaprevir	Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 R109K mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 R109K mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay	[PMID: 20176898]
Huh-7	EC₅₀	749 nM Compound: Telaprevir	Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 F43S mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 F43S mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay	[PMID: 20176898]
Huh-7	EC₅₀	886 nM Compound: Telaprevir	Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 V36M mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 V36M mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay	[PMID: 20176898]
Huh-7	EC₅₀	9631 nM Compound: Telaprevir	Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 R155G mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 R155G mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay	[PMID: 20176898]
Huh-7	EC₅₀	350 nM Compound: Telaprevir, VX-920	Antiviral activity against HCV 1B infected in human Huh7 cells by firefly luciferase reporter gene assay Antiviral activity against HCV 1B infected in human Huh7 cells by firefly luciferase reporter gene assay	[PMID: 20541424]
Huh-7	EC₅₀	540 nM Compound: Telaprevir	Antiviral activity against HCV 1b infected in Huh7 cells assessed as inhibition of viral replication after 72 hrs by RT-PCR Antiviral activity against HCV 1b infected in Huh7 cells assessed as inhibition of viral replication after 72 hrs by RT-PCR	[PMID: 20823284]
Huh-7	EC₅₀	700 nM Compound: Telaprevir	Antiviral activity against HCV 1a infected in Huh7 cells assessed as inhibition of viral replication after 72 hrs by RT-PCR Antiviral activity against HCV 1a infected in Huh7 cells assessed as inhibition of viral replication after 72 hrs by RT-PCR	[PMID: 20823284]
Huh-7	CC₅₀	37 μM Compound: Telaprevir	Cytotoxicity activity against human HuH7 cells by MTT assay Cytotoxicity activity against human HuH7 cells by MTT assay	[PMID: 20823284]
Huh-7	EC₅₀	176.2 nM Compound: VX-950	Antiviral activity against HCV1b harboring Q80Q polymorphism in NS3 protease gene infected in human Huh7/Lunet cells assessed as inhibition of viral replication after 3 days by luciferase based transient-transfection assay Antiviral activity against HCV1b harboring Q80Q polymorphism in NS3 protease gene infected in human Huh7/Lunet cells assessed as inhibition of viral replication after 3 days by luciferase based transient-transfection assay	[PMID: 20855726]
Huh-7	EC₅₀	376.7 nM Compound: VX-950	Antiviral activity against HCV1b Con1 harboring NS3 protease gene infected in human Huh7/Lunet cells assessed as inhibition of viral replication after 3 days by luciferase based transient-transfection assay Antiviral activity against HCV1b Con1 harboring NS3 protease gene infected in human Huh7/Lunet cells assessed as inhibition of viral replication after 3 days by luciferase based transient-transfection assay	[PMID: 20855726]
Huh-7	EC₅₀	72 nM Compound: VX-950	Antiviral activity against HCV1b harboring Q80K polymorphism in NS3 protease gene infected in human Huh7/Lunet cells assessed as inhibition of viral replication after 3 days by luciferase based transient-transfection assay Antiviral activity against HCV1b harboring Q80K polymorphism in NS3 protease gene infected in human Huh7/Lunet cells assessed as inhibition of viral replication after 3 days by luciferase based transient-transfection assay	[PMID: 20855726]
Huh-7	CC₅₀	37.46 μM Compound: Telaprevir	Cytotoxicity against human Huh7.5 cells after 96 hrs by MTT assay Cytotoxicity against human Huh7.5 cells after 96 hrs by MTT assay	[PMID: 23999140]
Huh-7	IC₅₀	<0.14 μM Compound: Telaprevir	Antiviral activity against HCV expressing pFL-J6/JFH/JC1 infected in human Huh7.5 cells assessed as inhibition of viral RNA synthesis after 96 hrs by one-step RT-PCR analysis Antiviral activity against HCV expressing pFL-J6/JFH/JC1 infected in human Huh7.5 cells assessed as inhibition of viral RNA synthesis after 96 hrs by one-step RT-PCR analysis	[PMID: 23999140]
Huh-7	CC₅₀	>10 μM Compound: 2, Incivek	Cytotoxicity against human HuH7 cells Cytotoxicity against human HuH7 cells	[PMID: 24135727]
Huh-7	EC₅₀	0.4 μM Compound: 2, Incivek	Antiviral activity against Hepatitis C virus infected in human HuH7 cells assessed as viral RNA replication Antiviral activity against Hepatitis C virus infected in human HuH7 cells assessed as viral RNA replication	[PMID: 24135727]
Huh-7	EC₅₀	350 nM Compound: Incivek	Antiviral activity against Hepatitis C virus genotype 1b infected in human HuH7 cells by subgenomic replicon-based luciferase assay Antiviral activity against Hepatitis C virus genotype 1b infected in human HuH7 cells by subgenomic replicon-based luciferase assay	[PMID: 24900813]
Huh-7	CC₅₀	>20 μM Compound: telaprevir	Cytotoxicity against human HuH7 cells expressing luciferase reporter gene after 3 days by WST-8 assay Cytotoxicity against human HuH7 cells expressing luciferase reporter gene after 3 days by WST-8 assay	[PMID: 24900815]
Huh-7	EC₅₀	0.45 μM Compound: telaprevir	Antiviral activity against HCV1b infected in human HuH7 cells expressing luciferase reporter gene assessed as reduction of luciferase activity after 3 days Antiviral activity against HCV1b infected in human HuH7 cells expressing luciferase reporter gene assessed as reduction of luciferase activity after 3 days	[PMID: 24900815]
Huh-7	CC₅₀	>20 μM Compound: Telaprevir	Cytotoxicity against human HuH7 cells after 3 days by tetrazolium dye method Cytotoxicity against human HuH7 cells after 3 days by tetrazolium dye method	[PMID: 26483202]
Huh-7	EC₅₀	0.36 μM Compound: Telaprevir	Antiviral activity against HCV genotype 1b infected in human HuH7 cells after 3 days by luciferase reporter gene assay Antiviral activity against HCV genotype 1b infected in human HuH7 cells after 3 days by luciferase reporter gene assay	[PMID: 26483202]
Huh-7	CC₅₀	47.83 μM Compound: VX-950	Cytotoxicity against human Huh7.5 cells Cytotoxicity against human Huh7.5 cells	[PMID: 26551513]
Huh-7	EC₅₀	0.129 μM Compound: VX-950	Antiviral activity against chimeric HCV FL-J6/JFH/JC1 infected in human Huh7.5 cells assessed as reduction of intracellular viral RNA level after 72 hrs by RT-PCR assay Antiviral activity against chimeric HCV FL-J6/JFH/JC1 infected in human Huh7.5 cells assessed as reduction of intracellular viral RNA level after 72 hrs by RT-PCR assay	[PMID: 26551513]
Huh-7	EC₅₀	720 nM Compound: Telaprevir	Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human Huh7 cells assessed as decrease in subgenomic RNA level after 72 hrs by RT-PCR analysis Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human Huh7 cells assessed as decrease in subgenomic RNA level after 72 hrs by RT-PCR analysis	10.1039/C1MD00227A
Huh-7.5	CC₅₀	23.7 μM Compound: VX-950; HY-10235	Cytotoxicity against human Huh7.5 cells assessed as inhibition of cell growth measured after 96 hrs by MTT assay Cytotoxicity against human Huh7.5 cells assessed as inhibition of cell growth measured after 96 hrs by MTT assay	[PMID: 34883293]
RD	CC₅₀	83.21 μM Compound: Telaprevir	Cytotoxicity against human RD cells assessed as reduction in cell viability by neutral red staining based CPE assay Cytotoxicity against human RD cells assessed as reduction in cell viability by neutral red staining based CPE assay	[PMID: 37857371]

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 402957-28-2
Appearance Solid
Molecular Weight 679.85
Formula C₃₆H₅₃N₇O₆
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
Synonyms

VX-950
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

Publications (44)

All WBCell Proliferation/Viability Assay

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Journal Impact Factor

Signal Transduct Target Ther

Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. [Abstract]

2021 May 29;6(1):212. PMID: 34052830
Nat Commun

Both Boceprevir and GC376 efficaciously inhibit SARS-CoV-2 by targeting its main protease. [Abstract]

2020 Sep 4;11(1):4417. PMID: 32887884
Nat Commun

Small molecule degraders of the hepatitis C virus protease reduce susceptibility to resistance mutations. [Abstract]

2019 Aug 1;10(1):3468. PMID: 31371704
Acta Pharm Sin B

Up-regulation of glycolipid transfer protein by bicyclol causes spontaneous restriction of hepatitis C virus replication. [Abstract]

2019 Jul;9(4):769-781. PMID: 31384537
ACS Cent Sci

Evaluation of SARS-CoV-2 Main Protease Inhibitors Using a Novel Cell-Based Assay. [Abstract]

2022 Feb 23;8(2):192-204. PMID: 35229034
J Med Chem

2-((4-Arylpiperazin-1-yl)methyl)benzonitrile Derivatives as Orally Available Inhibitors of Hepatitis C Virus with a Novel Mechanism of Action. [Abstract]

2020 Jun 11;63(11):5972-5989. PMID: 32378892
J Med Chem

Design and Synthesis of Cajanine Analogues against Hepatitis C Virus through Down-Regulating Host Chondroitin Sulfate N-Acetylgalactosaminyltransferase 1. [Abstract]

2016 Nov 23;59(22):10268-10284. PMID: 27783522
Int J Radiat Oncol Biol Phys

Targeting Phosphatidylinositol 4-Kinase IIIα for Radiosensitization: A Potential Model of Drug Repositioning Using an Anti-Hepatitis C Viral Agent. [Abstract]

2016 Nov 15;96(4):867-876. PMID: 27788957
Elife

Coagulation factors directly cleave SARS-CoV-2 spike and enhance viral entry. [Abstract]

2022 Mar 23:11:e77444. PMID: 35294338
Eur J Med Chem

Synthesis and structure-activity relationship study of new biaryl amide derivatives and their inhibitory effects against hepatitis C virus. [Abstract]

2022 Jan 15:228:114033. PMID: 34883293
Eur J Med Chem

Discovery and evolution of aloperine derivatives as a new family of HCV inhibitors with novel mechanism. [Abstract]

2018 Jan 1:143:1053-1065. PMID: 29232582

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.
Pharmaceutics

Activation of Tenofovir Alafenamide and Sofosbuvir in the Human Lung and Its Implications in the Development of Nucleoside/Nucleotide Prodrugs for Treating SARS-CoV-2 Pulmonary Infection. [Abstract]

2021 Oct 11;13(10):1656. PMID: 34683949
Cells

Viral Interference of Hepatitis C and E Virus Replication in Novel Experimental Co-Infection Systems. [Abstract]

2022 Mar 8;11(6):927. PMID: 35326378
Int J Mol Sci

Discovery of TRPV4-Targeting Small Molecules with Anti-Influenza Effects Through Machine Learning and Experimental Validation. [Abstract]

2025 Feb 6;26(3):1381. PMID: 39941149
Eur J Pharmacol

Aloperine inhibits hepatitis C virus entry into cells by disturbing internalisation from endocytosis to the membrane fusion process. [Abstract]

2020 Sep 15;883:173323. PMID: 32622669
Eur J Pharmacol

Farnesoid X receptor agonist GW4064 indirectly inhibits HCV entry into cells via down-regulating scavenger receptor class B type I. [Abstract]

2019 Jun 15:853:111-120. PMID: 30902657
Int J Antimicrob Agents

Efficacy of antiretroviral compounds against Toxoplasma gondii in vitro. [Abstract]

2019 Dec;54(6):814-819. PMID: 31479744
Antimicrob Agents Chemother

Effects of Antiviral Drugs on Organic Anion Transport in Human Placental BeWo Cells. [Abstract]

2015 Dec;59(12):7666-7670. PMID: 26416870

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.
Antimicrob Agents Chemother

Cyclophilin and NS5A inhibitors, but not other anti-hepatitis C virus (HCV) agents, preclude HCV-mediated formation of double-membrane-vesicle viral factories. [Abstract]

2015 May;59(5):2496-507. PMID: 25666154
Antimicrob Agents Chemother

The combination of alisporivir plus an NS5A inhibitor provides additive to synergistic anti-hepatitis C virus activity without detectable cross-resistance. [Abstract]

2014 Jun;58(6):3327-34. PMID: 24687498
J Gen Virol

Induction of selective autophagy in cells replicating hepatitis C virus genome. [Abstract]

2018 Dec;99(12):1643-1657. PMID: 30311874
Antiviral Res

Long-chain fatty acyl-coenzyme A suppresses hepatitis C virus infection by targeting virion-bound lipoproteins. [Abstract]

2020 May;177:104734. PMID: 32057770
Antiviral Res

Sofosbuvir inhibits hepatitis A virus replication in vitro assessed by a cell-based fluorescent reporter system. [Abstract]

2018 Jun:154:51-57. PMID: 29653132
Antiviral Res

A natural small molecule inhibitor corilagin blocks HCV replication and modulates oxidative stress to reduce liver damage. [Abstract]

2018 Feb:150:47-59. PMID: 29224736
Antiviral Res

Avasimibe: A novel hepatitis C virus inhibitor that targets the assembly of infectious viral particles. [Abstract]

2017 Dec:148:5-14. PMID: 29074218
Antiviral Res

Identification of a lead like inhibitor of the hepatitis C virus non-structural NS2 autoprotease. [Abstract]

2015 Dec;124:54-60. PMID: 26518228

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.
Antiviral Res

Epoxide based inhibitors of the hepatitis C virus non-structural 2 autoprotease. [Abstract]

2015 May;117:20-6. PMID: 25703928
Sci Rep

Hepatitis C virus NS3/4A inhibitors and other drug-like compounds as covalent binders of SARS-CoV-2 main protease. [Abstract]

2022 Jul 16;12(1):12197. PMID: 35842458
Sci Rep

CD36 is a co-receptor for hepatitis C virus E1 protein attachment. [Abstract]

2016 Feb 22;6:21808. PMID: 26898231

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).
Sci Rep

Small molecule inhibitors of HCV replication from pomegranate. [Abstract]

2014 Jun 24;4:5411. PMID: 24958333
Chem Res Toxicol

Activation of inflammasomes by agents causing idiosyncratic skin reactions: a possible biomarker. [Abstract]

2014 Jun 16;27(6):949-51. PMID: 24877608
Fungal Biol

The serine peptidase inhibitor N-ρ-tosyl-l-phenylalanine chloromethyl ketone (TPCK) affects the cell biology of Candida haemulonii species complex. [Abstract]

2021 May;125(5):378-388. PMID: 33910679
Biochimie

Crowded environment affects the activity and inhibition of the NS3/4A protease. [Abstract]

2020 Sep;176:169-180. PMID: 32717410
Bioorg Med Chem

Harzianoic acids A and B, new natural scaffolds with inhibitory effects against hepatitis C virus. [Abstract]

2019 Feb 1;27(3):560-567. PMID: 30606673
PLoS One

Cyclophilin Inhibitors Remodel the Endoplasmic Reticulum of HCV-Infected Cells in a Unique Pattern Rendering Cells Impervious to a Reinfection. [Abstract]

2016 Jul 21;11(7):e0159511. PMID: 27442520
PLoS One

Characterization of the Anti-HCV Activities of the New Cyclophilin Inhibitor STG-175. [Abstract]

2016 Apr 22;11(4):e0152036. PMID: 27104614
PLoS One

Conditional Inducible Triple-Transgenic Mouse Model for Rapid Real-Time Detection of HCV NS3/4A Protease Activity. [Abstract]

2016 Mar 4;11(3):e0150894. PMID: 26943641
Virology

Human pegivirus (GB virus C) NS3 protease activity inhibits induction of the type I interferon response and is not inhibited by HCV NS3 protease inhibitors. [Abstract]

2014 May;456-457:300-9. PMID: 24889249

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.
Biomed Res Int

A Simple but Accurate Method for Evaluating Drug-Resistance in Infectious HCVcc System. [Abstract]

2017:2017:1236801. PMID: 28904942

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.
bioRxiv

2023 Nov 5.
Bioemas

2020 Apr.
Personalized Medicine Universe

2019 May.
Seoul National University

2016 Aug.
Open Virol J

Both Cyclophilin Inhibitors and Direct-Acting Antivirals Prevent PKR Activation in HCV-Infected Cells. [Abstract]

2014 Mar 7;8:1-8. PMID: 24799968

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.

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.4709 mL

7.3546 mL

14.7091 mL

5 mM

0.2942 mL

1.4709 mL

2.9418 mL

10 mM

0.1471 mL

0.7355 mL

1.4709 mL

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Protocol

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].

MedChemExpress (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.

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (290 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Portuguese - PT (392 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Lin K, et al. VX-950, a novel hepatitis C virus (HCV) NS3-4A protease inhibitor, exhibits potent antiviral activities in HCv replicon cells. Antimicrob Agents Chemother. 2006 May;50(5):1813-22. [Content Brief]

[2]. Perni RB, et al. Preclinical profile of VX-950, a potent, selective, and orally bioavailable inhibitor of hepatitis C virus NS3-4A serine protease. Antimicrob Agents Chemother. 2006 Mar;50(3):899-909. [Content Brief]

[3]. Zhang X, et al. Discovery and evolution of aloperine derivatives as a new family of HCV inhibitors with novel mechanism. Eur J Med Chem. 2018 Jan 1;143:1053-1065. [Content Brief]

[4]. Qi Sun, et al. Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. Signal Transduct Target Ther. 2021 May 29;6(1):212. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

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Telaprevir

Anti-Infection Compound Library

Metabolism/Protease Compound Library

FDA-Approved Drug Library

Antiviral Compound Library

Drug Repurposing Compound Library

Covalent Screening Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Hepatitis C Virus Compound Library

Targeted Diversity Library

EMA-Approved Drug Library

Human Metabolite Library

Heterocyclic Compound Library

Withdrawn Drug Compound Library

Off-patent Drug Library

Protease Inhibitor Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Nephrotoxicity Compound Library

Publications Citing Use of MedChemExpress (MCE) Telaprevir

Biological Activity

Chemical Information

Publications (44)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Telaprevir

Anti-Infection Compound Library

Metabolism/Protease Compound Library

FDA-Approved Drug Library

Antiviral Compound Library

Drug Repurposing Compound Library

Covalent Screening Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Hepatitis C Virus Compound Library

Targeted Diversity Library

EMA-Approved Drug Library

Human Metabolite Library

Heterocyclic Compound Library

Withdrawn Drug Compound Library

Off-patent Drug Library

Protease Inhibitor Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Nephrotoxicity Compound Library

Publications Citing Use of MedChemExpress (MCE) Telaprevir

Biological Activity

Chemical Information

Publications (44)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Telaprevir Related Classifications

Cat. No.: HY-10235