Bay 41-4109 racemate

SKU: orb1225400

Description

The racemate form of Bay 41-4109, which is a potent, non-nucleosidic inhibitor of HBV nucleocapsid maturation with IC50 of 0.05 uM.

Key Properties

• CAS Number: 298708-79-9
• MW: 395.7629296
• Purity: >98% (HPLC)
• Formula: C₁₈H₁₃ClF₃N₃O₂
• SMILES: CC1=C(C(N=C(N1)C2=C(C=C(C=N2)F)F)C3=C(C=C(C=C3)F)Cl)C(=O)OC
• Target: HBV
• Solubility: DMSO: ≥ 37 mg/mL

Bioactivity

• In Vivo:
  BAY 41-4109 reduces viral DNA in the liver and in the plasma dose-dependently with efficacy comparable to 3TC. BAY 41-4109 reduces hepatitis B virus core antigen (HBcAg) in livers of HBV-transgenic mice. Pharmacokinetic studies in mice have shown rapid absorption, a bioavailability of 30% and dose-proportional plasma concentrations, about 60% in rats and dogs. BAY41-4109 inhibits virus production In vivo by a mechanism that targets the viral capsid.
• In Vitro:
  BAY 41-4109 is able to both accelerate and misdirect capsid assembly in vitro. Preformed capsids are stabilized by BAY 41-4109, up to a ratio of one inhibitor molecule per two dimers. BAY 41-4109 is equally effective at inhibiting HBV DNA release and the cytoplasmic HBcAg level, with IC50s of 32.6 and 132 nM in HepG2.2.15 cells, respectively. HBV DNA and HBcAg are inhibited in a dose-dependent manner, indicating that the anti-HBV mechanisms are associated with and dependent on the rate of HBcAg inhibition.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Bay-414109 racemate

Quick Database Links

Gene Symbol

HBV