Nesbuvir

SKU: orb1679055

Description

Nesbuvir is a potent and selective inhibitor of the HCV NS5B RNA-dependent RNA polymerase. It demonstrates high antiviral activity in vitro, with an IC50 of 9 nM against HCV genotype 1b replicons in hepatocellular carcinoma cells, supporting its use in hepatitis C virology and antiviral discovery research.

Research Area

Infectious Disease & Virology, Protein Biochemistry

Key Properties

• CAS Number: 691852-58-1
• MW: 446.49
• Purity: 99.99% (May vary between batches)
• Formula: C₂₂H₂₃FN₂O₅S
• SMILES: CNC(=O)c1c(oc2cc(N(CCO)S(C)(=O)=O)c(cc12)C1CC1)-c1ccc(F)cc1
• Target: HCV Protease
• Solubility: DMSO:45 mg/mL (100.79 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.48 mM)

Bioactivity

• Target IC50:
  NS3V170A:13 nM (EC50)|NS3V170A:9 nM (EC50)|NS3K583T:15 nM (EC50)|NS5B:5 nM|NS5BI424V:13 nM (EC50)
• In Vivo:
  Nesbuvir is demonstrated to yield significant antiviral effects in mice with chimeric human livers and in patients infected with HCV. 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.
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• 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. 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.
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• 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 .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Nesbuvir, NS5B polymerase, HCV 796, HCV NS5B polymerase, HCV Protease, HCVProtease, HCV796, HCV-796

Compound Identifiers

PubChem CID

11561383