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Microbiology&virology HCV Protease Nesbuvir

Nesbuvir

Catalog No. TQ0090   CAS 691852-58-1
Synonyms: HCV-796
Purity 98.00%

Nesbuvir (HCV-796) is a nonnucleoside inhibitor of the HCV nonstructural protein 5B (NS5B) polymerase.

Nesbuvir, CAS 691852-58-1
Pack Size Availability Price/USD Quantity
10 mg Inquiry 414.00
25 mg Inquiry 839.00
50 mg Inquiry 1379.00
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Purity 98.00%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Nesbuvir (HCV-796) is a nonnucleoside inhibitor of the HCV nonstructural protein 5B (NS5B) polymerase.
Targets&IC50
In vitro Replicon cells are treated with 1 mg/mL G418 and combinations of the two compounds. Nesbuvir is added to 40 or 80 nM (approximately 10 and 20 times the EC50 in a 3-day replicon inhibition assay, respectively) and Boceprevir is added to 400 or 800 nM (approximately 2 and 4 times the EC50, respectively). The EC50s for Nesbuvir and Boceprevir for the parental replicon in the transient expression assay are comparable to those obtained in the 3-day inhibition assay with the stable replicon cells; the EC50 for Nesbuvir in the transient expression assay is 14 nM, whereas it is 5 nM for the stable replicon [1].
In vivo Nesbuvir is demonstrated to yield significant antiviral effects in mice with chimeric human livers and in patients infected with HCV [2].
Cell Research
Huh7-BB7 cells are seeded at a density of 20,000 cells per 100 mm dish in DMEM supplemented with 2% FBS, 1 mg/mL G418, and various concentrations of Nesbuvir and/or Boceprevir with DMSO at a final concentration of 0.5% (vol/vol). The medium is removed and is replaced with a fresh medium with the appropriate compound concentrations every 3 or 4 days. After 7 days, the cells are split 1 to 10, placed into fresh 100 mm dishes, and incubated with medium with the appropriate compound concentrations. After 20 days, the medium is removed and the cells are fixed with 7% (wt/vol) formaldehyde and stained with 1% (wt/vol) crystal violet in 50% (vol/vol) ethanol [1].

Description

Nesbuvir (HCV-796) is a nonnucleoside inhibitor of the HCV nonstructural protein 5B (NS5B) polymerase.

Targets&IC50

In Vitro

Replicon cells are treated with 1 mg/mL G418 and combinations of the two compounds. Nesbuvir is added to 40 or 80 nM (approximately 10 and 20 times the EC50 in a 3-day replicon inhibition assay, respectively) and Boceprevir is added to 400 or 800 nM (approximately 2 and 4 times the EC50, respectively). The EC50s for Nesbuvir and Boceprevir for the parental replicon in the transient expression assay are comparable to those obtained in the 3-day inhibition assay with the stable replicon cells; the EC50 for Nesbuvir in the transient expression assay is 14 nM, whereas it is 5 nM for the stable replicon [1].

In Vivo

Nesbuvir is demonstrated to yield significant antiviral effects in mice with chimeric human livers and in patients infected with HCV [2].

Cell Research

Huh7-BB7 cells are seeded at a density of 20,000 cells per 100 mm dish in DMEM supplemented with 2% FBS, 1 mg/mL G418, and various concentrations of Nesbuvir and/or Boceprevir with DMSO at a final concentration of 0.5% (vol/vol). The medium is removed and is replaced with a fresh medium with the appropriate compound concentrations every 3 or 4 days. After 7 days, the cells are split 1 to 10, placed into fresh 100 mm dishes, and incubated with medium with the appropriate compound concentrations. After 20 days, the medium is removed and the cells are fixed with 7% (wt/vol) formaldehyde and stained with 1% (wt/vol) crystal violet in 50% (vol/vol) ethanol [1].

Synonyms HCV-796
Purity 98.00%
Appearance solid
Molecular Weight 446.49
Formula C22H23FN2O5S
CAS No. 691852-58-1

Storage

-20℃ 3 years powder

-80℃ 2 years in solvent

Solubility Information

:

DMSO: ≥50mg/mL(111.98 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Flint M, et al. Selection and characterization of hepatitis C virus replicons dually resistant to the polymerase and protease inhibitors HCV-796 and boceprevir (SCH 503034). Antimicrob Agents Chemother. 2009 Feb;53(2):401-11. 2. Reich S, et al. Mechanisms of activity and inhibition of the hepatitis C virus RNA-dependent RNA polymerase. J Biol Chem. 2010 Apr 30;285(18):13685-93.

Related Products

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R-1479 VCH-916 Nesbuvir Tomeglovir Syrosingopine Platycodin D3 Glycyrin gamma-Fagarine

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