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Telaprevir (VX-950)

Telaprevir (VX-950)

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Protocol(Only for Reference)

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Preparing Stock Solutions

Research Area

Customer Reviews (1)

Product Citations (6)

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Biological Activity

Protocol(Only for Reference)

Chemical Information

Preparing Stock Solutions

Research Area

Customer Reviews (1)

Product Citations (6)

Tech Support & FAQs

Choose Your Country or Region

Biological Activity

Protocol(Only for Reference)

Chemical Information

Preparing Stock Solutions

Research Area

Customer Reviews (1)

Product Citations (6)

Tech Support & FAQs

E-newsletter

Product Citations(6)

Customer Reviews(1) in vivo invitation

Quality Control & MSDS

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

Kinase Assay: ^[1]

Cell Assay: ^[1]

Animal Study: ^[2]

References

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

Related HCV Protease Inhibitors

Product Citations(6)

Customer Reviews(1) in vivo invitation

Quality Control & MSDS

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

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Research Area

Kinase Assay: ^[1]

Cell Assay: ^[1]

Animal Study: ^[2]

References

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

Related HCV Protease Inhibitors

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Product Citations(6)

Customer Reviews(1) in vivo invitation

Quality Control & MSDS

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

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Research Area

Kinase Assay: [1]

Cell Assay: [1]

Animal Study: [2]

References

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

Related HCV Protease Inhibitors

Recently Viewed Items

Kinase Assay: ^[1]

Cell Assay: ^[1]

Animal Study: ^[2]

Antimicrob Agents Chemother,2012, 56(7):3888-97

Antiviral Res,2013, 99(1):6-11

PLoS One,2013, 8(12):e82094

Virology,2012, 435(2):385-94

BMC Res Notes,2013, 6(1):445
PLoS One,2013, 8(12):e82299

Inhibitor Library Bioactive Compound Library

Compare HCV Protease Inhibitors

Research Area
Research Area
Dr. Antonino Maria Sparta demonstrates a breakthrough in leukemia research by utilizing two inhibitors produced by Selleck Chemicals.

Cat.No.	Product Name	Solubility (25°C)
S1482	Daclatasvir (BMS-790052)	<1 mg/mL	148 mg/mL	148 mg/mL
S1183	Danoprevir (ITMN-191)	<1 mg/mL	144 mg/mL	144 mg/mL
S1538	Telaprevir (VX-950)	<1 mg/mL	136 mg/mL	<1 mg/mL
S1480	VX-222 (VCH-222, Lomibuvir)	<1 mg/mL	89 mg/mL	89 mg/mL

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

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

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 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 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

1

Download Telaprevir (VX-950) SDF

Molecular Weight (MW)	679.85
Formula	C₃₆H₅₃N₇O₆
CAS No.	402957-28-2
Synonyms	N/A

Solubility (25°C) * <1 mg/ml means slightly soluble or insoluble DMSO 136 mg/mL (200 mM) Water <1 mg/mL (<1 mM) Ethanol <1 mg/mL (<1 mM)
Storage	2 years -20°CPowder
Storage	6 months-80°Cin DMSO

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

Stock Solution (1ml DMSO)	1mM	10mM	20mM	30mM
Mass(mg)	0.67985	6.7985	13.597	20.3955

Molarity Calculator Dilution Calculator Molecular Weight Calculator

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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.

The cyclophilin inhibitor SCY-635 disrupts hepatitis C virus NS5A-cyclophilin A complexes. [Hopkins S, et al. Antimicrob Agents Chemother 2012;56(7):3888-97]
PubMed: 22585215
Development of a multiplex phenotypic cell-based high throughput screening assay to identify novel hepatitis C virus antivirals. [Kim HY, et al. Antiviral Res 2013;99(1):6-11]
PubMed: 23660623
Hepatitis C Virus NS3/4A Protease Inhibits Complement Activation by Cleaving Complement Component 4 [Seiichi Mawatari,et al. PLoS One 2013;8(12):e82094]
PubMed: 24349192

DDB1 is a cellular substrate of NS3/4A protease and required for hepatitis C virus replication. [Kang X, et al. Virology 2012;435(2):385-94]
PubMed: 23137809
Biochemical interaction of anti-HCV telaprevir with the ABC transporters P-glycoprotein and breast cancer resistance protein. [Fujita Y, et al. BMC Res Notes 2013;6(1):445]
PubMed: 24196382
Inhibitory effects of caffeic Acid phenethyl ester derivatives on replication of hepatitis C virus. [Shen H ,et al. PLoS One 2013;8(12):e82299]
PubMed: 24358168

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.
Bortezomib (PS-341)
Bortezomib (PS-341) is a potent 20S proteasome inhibitor with K_i 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.
Emtricitabine
Emtricitabine (Emtriva) is a nucleoside reverse transcriptase inhibitor with an IC50 of 27.7 μM.
Nilotinib (AMN-107)
Nilotinib (AMN-107) is a Bcr-Abl inhibitor with IC50 less than 30 nM.

Features:A selective inhibitor of native and mutant Bcr-Abl.

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 9:00 AM - 20:00 PM (EST)

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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).
Oprozomib (ONX 0912)
Oprozomib (ONX 0912) is an orally bioavailable inhibitor for CT-L activity of 20S proteasome β5/LMP7 with IC50 of 36 nM/82 nM.
Batimastat (BB-94)
Batimastat (BB-94) is a potent, broad spectrum matrix metalloprotease (MMP) inhibitor for MMP-1, MMP-2, MMP-9, MMP-7 and MMP-3 with IC50 of 3 nM, 4 nM, 4 nM, 6 nM and 20 nM, respectively.
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.
Telaprevir (VX-950)
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.
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.
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).
Bortezomib (PS-341)
Bortezomib (PS-341) is a potent 20S proteasome inhibitor with K_i of 0.6 nM.
MG-132
MG-132 is an inhibitor of proteasome with IC50 of 100 nM, and also inhibits calpain with IC50 of 1.2 μM.
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.

Cat.No.	Product Name	Solubility (25°C)
Cat.No.	Product Name	Water	DMSO	Ethanol
S1482	Daclatasvir (BMS-790052)	<1 mg/mL	148 mg/mL	148 mg/mL
S1183	Danoprevir (ITMN-191)	<1 mg/mL	144 mg/mL	144 mg/mL
S1538	Telaprevir (VX-950)	<1 mg/mL	136 mg/mL	<1 mg/mL
S1480	VX-222 (VCH-222, Lomibuvir)	<1 mg/mL	89 mg/mL	89 mg/mL

Description

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

HCV NS3-4A serine protease

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]

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]

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.