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Telaprevir

Catalog No. T6190   CAS 402957-28-2
Synonyms: VX-950, LY-570310, Incivek, MP-424

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

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Telaprevir Chemical Structure
Telaprevir, CAS 402957-28-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 44.00
5 mg In stock $ 97.00
10 mg In stock $ 162.00
25 mg In stock $ 259.00
50 mg In stock $ 358.00
100 mg In stock $ 657.00
1 mL * 10 mM (in DMSO) In stock $ 179.00
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Purity: 96.9%
Purity: 96.33%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Telaprevir (Incivek) (VX-950) is an effective inhibitor of HCV NS3-4A serine protease (IC50: 0.35 μM).
Targets&IC50 HCV NS3-4A serine protease:0.35 μM
In vitro In a mouse model, Telaprevir administration at doses of 10 and 25 mg/kg (p.o.) reduced hepatitis C virus protease-dependent cleavage (18.7%) and secretion of SEAP (18.4%) from the liver to the bloodstream. In mice with genotype 1b HCV-infected human hepatocytes, a one-week treatment with Telaprevir at 200 mg/kg resulted in a decrease in HCV RNA levels. Furthermore, when used in combination with MK-0608 at a dose of 50 mg/kg over four weeks, this regimen completely eliminated the virus from the mice.
In vivo Telaprevir (17.5 μM) effectively eradicates HCV RNA in replicating cells, with no recurrence observed 13 days post-treatment. When used in combination with IFN-α, Telaprevir moderately enhances the synergistic effect, reducing HCV RNA replication and inhibiting resistance mutations without significant toxicity. The compound exhibits a time-dependent increase in inhibitory efficacy against HCV RNA replication, with IC50 values of 0.574 μM, 0.488 μM, 0.210 μM, and 0.139 μM at 24, 48, 72, and 120 hours, respectively. In Con1 (genotype 1b) subgenomic HCV replicon cells, Telaprevir inhibits the HCV NS3-4A serine protease, suppressing viral polyprotein processing and consequently diminishing all HCV RNA and protein levels in a time and dose-dependent manner. Additionally, Telaprevir shows no toxicity in HCV replicating cells or parent Huh-7 and HepG2 cells after 48 hours of treatment.
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 Cells are incubated with various concentrations of Telaprevir for 48 hours. Cell viability is determined by using a tetrazolium (MTS)-based cell viability assay.(Only for Reference)
Synonyms VX-950, LY-570310, Incivek, MP-424
Molecular Weight 679.85
Formula C36H53N7O6
CAS No. 402957-28-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 125 mg/mL (183.9 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

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. 3. Ohara E, et al. J Hepatol, 2011, 54(5), 872-878.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Anti-Cancer Approved Drug Library Human Metabolite Library Immunology/Inflammation Compound Library ReFRAME Related Library Anti-Liver Cancer Compound Library Anti-Infection Compound Library FDA-Approved & Pharmacopeia Drug Library Clinical Compound Library

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Keywords

Telaprevir 402957-28-2 Microbiology/Virology Proteases/Proteasome SARS-CoV HCV Protease Inhibitor Hepatitis C virus LY570310 VX950 SARS coronavirus MP424 VX-950 LY 570310 VX 950 HCV LY-570310 Incivek MP-424 inhibit MP 424 inhibitor

 

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