| Description | Bay 41-4109 less active enantiomer shows less activity than Bay 41-4109. BAY 41-4109 is a potent HBV inhibitor (IC50: 53 nM). |
| 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 [2]. In HepG2.2.15 cells, BAY 41-4109 is equally effective at inhibiting HBV DNA release and the cytoplasmic HBcAg level (IC50s: 32.6 and 132 nM). HBV DNA and HBcAg are inhibited in a dose-dependent manner [3]. |
| 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 the 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 [1]. BAY41-4109 inhibits virus production in vivo by a mechanism that targets the viral capsid [2]. |
| Target activity | HBV:53 nM |
| molecular weight | 395.76 |
| Molecular formula | C18H13ClF3N3O2 |
| CAS | 476617-51-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 37 mg/mL (93.49 mM) |
| References | 1. Weber O, et al. Inhibition of human hepatitis B virus (HBV) by a novel non-nucleosidic compound in a transgenic mouse model. Antiviral Res. 2002 May;54(2):69-78. 2. Stray SJ, et al. BAY 41-4109 has multiple effects on Hepatitis B virus capsid assembly. J Mol Recognit. 2006 Nov-Dec;19(6):542-8. 3. Wu GY, et al. Inhibition of hepatitis B virus replication by Bay 41-4109 and its association with nucleocapsid disassembly. J Chemother. 2008 Aug;20(4):458-67. |