AT-130

AT-130, a phenylpropenamide derivative, is a potent hepatitis B virus (HBV) replication non-nucleoside inhibitor. AT-130 inhibits the viral DNA synthesis with an IC50 of 0.13 uM. AT-130 inhibits both wt and mutant HBVs. AT-130 has anti-HBV activity in hepatoma cells[1][2][3].

AT-130 inhibits Wt HBV (IC50=2.4 µM), rtL180M HBV (IC50=9.8 µM), rtM204I HBV (IC50=35.6 µM)[1]. AT-130 (0.1, 1, 5, 10, 100 uM; for 7 days) causes dose-dependent inhibition of wt HBV replication in HepG2 cells transduced with HBV baculovirus. AT-130 at a concentration of 2.5 uM, reduces encapsidated HBV DNA by 50% (IC50) and at 18.5 uM by 90% (IC90)[1]. AT-130 has no toxic to either HepG2 or Huh-7 cells at concentrations of up to 250 µM[1]. AT-130 (0.005, 0.05, 0.5, 5, 50 uM) does not inhibit HBV DNA synthesis by blocking the HBV endogenous DNA polymerase reaction directly in Huh 7 or HepG2 cells. AT-130 inhibits HBV DNA replication in hepatoma cells but has no effect on viral DNA polymerase activity or core protein translation[3]. AT-130 (2.5, 18.5 uM) has no effect on total HBV RNA production but does reduce encapsidated RNA. AT-130 does not affect core protein or nucleocapsid production and the activity of the protein expression vector[3].

References:
[1]. William E Delaney 4th, et al. Phenylpropenamide derivatives AT-61 and AT-130 inhibit replication of wild-type and lamivudine-resistant strains of hepatitis B virus in vitro. Antimicrob Agents Chemother. 2002 Sep;46(9):3057-60.
[2]. R B Perni , et al. Phenylpropenamide derivatives as inhibitors of hepatitis B virus replication. Bioorg Med Chem Lett. 2000 Dec 4;10(23):2687-90.
[3]. J J Feld, et al. The phenylpropenamide derivative AT-130 blocks HBV replication at the level of viral RNA packaging. Antiviral Res. 2007 Nov;76(2):168-77.