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Nesbuvir

Catalog No. TQ0090 CAS 691852-58-1

Synonyms: HCV-796

Nesbuvir is a selective hepatitis C virus (HCV) nonstructural protein 5B (NS5B) RNA-dependent polymerase inhibitor.Nesbuvir has an IC50 of 9 nM against hepatocellular carcinoma cells containing 1b HCV replicons.

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Nesbuvir, CAS 691852-58-1

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Purity: 98%

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Description	Nesbuvir is a selective hepatitis C virus (HCV) nonstructural protein 5B (NS5B) RNA-dependent polymerase inhibitor.Nesbuvir has an IC50 of 9 nM against hepatocellular carcinoma cells containing 1b HCV replicons.
Targets&IC50	NS5BI424V:13 nM (EC50), NS3V170A:13 nM (EC50), NS3K583T:15 nM (EC50), NS3V170A:9 nM (EC50), NS5B:5 nM
In vitro	Nesbuvir (40 or 80 nM) (approximately 10 and 20 times the EC50 in a 3-day replicon inhibition assay, respectively). The EC50 for Nesbuvir in the transient expression assay is 14 nM, whereas it is 5 nM for the stable replicon.[1] Nesbuvir (0.1 and 1 μM; Huh-7 cells; for 16 days) reduced about 3.6 log10 and 4.2 log10 HCV RNA levels, respectively.[3]
In vivo	Nesbuvir is demonstrated to yield significant antiviral effects in mice with chimeric human livers and in patients infected with HCV.[2] Nesbuvir (chimeric mouse model) treatment resulted in a 2.02 +/- 0.55 log reduction in HCV titer, whereas in combination with interferon using a suboptimal dose of 30 mg/kg three times per day showed a 2.44 log reduction and were better than interferon treatment only.[5]
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
Molecular Weight	446.49
Formula	C22H23FN2O5S
CAS No.	691852-58-1

Storage

keep away from direct sunlight

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 45.0 mg/mL (100.8 mM)

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

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;53(2):401-411. 2. Reich S, et al. Mechanisms of activity and inhibition of the hepatitis C virus RNA-dependent RNA polymerase. J Biol Chem. 2010;285(18):13685-13693. 3. Howe AY, et al. Molecular mechanism of hepatitis C virus replicon variants with reduced susceptibility to a benzofuran inhibitor, HCV-796. Antimicrob Agents Chemother. 2008;52(9):3327-3338. 4. Meshram RJ, et al. Effective epitope identification employing phylogenetic, mutational variability, sequence entropy, and correlated mutation analysis targeting NS5B protein of hepatitis C virus: from bioinformatics to therapeutics. J Mol Recognit. 2015;28(8):492-505. 5. Kneteman NM, et al. HCV796: A selective nonstructural protein 5B polymerase inhibitor with potent anti-hepatitis C virus activity in vitro, in mice with chimeric human livers, and in humans infected with hepatitis C virus. Hepatology. 2009;49(3):745-752.

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Nesbuvir 691852-58-1 Microbiology/Virology Proteases/Proteasome HCV Protease HCV-796 Inhibitor inhibitor inhibit

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