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Telaprevir

SKU: orb1300995

Description

Telaprevir

Research Area

Infectious Disease & Virology, Protein Biochemistry

Images & Validation

Key Properties

CAS Number402957-28-2
MW679.85
Purity98.89%
FormulaC36H53N7O6
SMILESCCC[C@H](NC(=O)[C@@H]1[C@H]2CCC[C@H]2CN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)c1cnccn1)C1CCCCC1)C(C)(C)C)C(=O)C(=O)NC1CC1
TargetHCV Protease,SARS-CoV
SolubilityEthanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:125 mg/mL (183.86 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+90% Corn Oil:3.3 mg/mL (4.85 mM)

Bioactivity

Target IC50
HCV NS3/4A serine protease:0.35 μM
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.
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.
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)

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

HCVProtease, HCV Protease, HCV NS3-4A serine protease, HCV, Hepatitis C virus, Incivek, MP424, MP-424, MP 424, inhibit, Inhibitor, LY 570310, LY570310, LY-570310, VX950, VX-950, SARSCoV, SARS-CoV, SARS coronavirus, Telaprevir, VX 950

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Key Properties

No computed properties available.

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Telaprevir (orb1300995)

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(Recommended: An additional animal making an allowance for loss during the experiment)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

1 mg
$ 90.00
5 mg
$ 140.00
10 mg
$ 210.00
1 ml x 10 mM (in DMSO)
$ 220.00
25 mg
$ 300.00
50 mg
$ 400.00
100 mg
$ 700.00
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