Lomibuvir

SKU: orb1300519

Description

Lomibuvir (VCH-222) is a potent, non-nucleoside allosteric inhibitor of the Hepatitis C virus NS5B RNA-dependent RNA polymerase, exhibiting high affinity with a Kd of 17 nM. It demonstrates strong antiviral activity in HCV subgenomic replicon assays (EC₅₀ = 5.2 nM) and preferentially blocks elongative RNA synthesis. This small molecule is a valuable tool for investigating HCV replication mechanisms in vitro.

Research Area

Cell Biology, Infectious Disease & Virology, Molecular Biology, Protein Biochemistry

Key Properties

• CAS Number: 1026785-55-6
• MW: 445.61
• Purity: 99.83% (May vary between batches)
• Formula: C₂₅H₃₅NO₄S
• SMILES: CC1CCC(CC1)C(=O)N(C1CCC(O)CC1)c1cc(sc1C(O)=O)C#CC(C)(C)C
• Target: HCV Protease,DNA/RNA Synthesis
• Solubility: Ethanol:82 mg/mL (184.02 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:82 mg/mL (184.02 mM)

Bioactivity

• Target IC50:
  HCV NS5B 1a:0.94-1.2 μM
• In Vivo:
  In rats and dogs, Lomibuvir displays fine pharmacokinetic prole, including low total body clearance and excellent oral bioavailability (greater than 30%) and good ADME properties. Lomibuvir is biotransformed by several enzymes (CYP1A1, 2A6, 2B6, 2C8, CYP 3A4, UGT1A3) and is predicted to be actively transported in liver and excreted mainly intact in bile or as glucuronide adducts.
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• In Vitro:
  Lomibuvir (VX-222) is an effective non-nucleoside, allosteric inhibitor of the hepatitis C virus NS5B polymerase, exhibiting strong clinical efficacy. It demonstrates potent inhibition against the wild-type HCV 1b/Con1 replicon with an EC50 of 5.2 nM and against mutant replicons M423T, L419M, and I482L with EC50s of 79.8, 563.1, and 45.3 nM, respectively. Besides slightly hindering de novo initiation, Lomibuvir prominently impairs primer extension, illustrated by an IC50 of 31 nM for primer-extended RNA synthesis.
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Storage & Handling

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

Alternative Names

DNA/RNA Synthesis, cis-isomer, cis-Lomibuvir, Lomibuvir, inhibit, non-nucleoside polymerase, Inhibitor, HCV Protease, HCVProtease, HCV NS5B 1a, HCV NS5B 1b, HCV, Hepatitis C virus, VCH222, VCH-222, VCH 222, VX 222, VX222, VX-222, RdRp

Compound Identifiers

PubChem CID

24798764