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 EC 50 of 0.13 μM. AT-130 inhibits both wt and mutant HBVs. AT-130 has anti-HBV activity in hepatoma cells . In Vitro AT-130 inhibits Wt HBV (IC 50 =2.4 μM), rtL180M HBV (IC 50 =9.8 μM), rtM204I HBV (IC 50 =35.6 μM). AT-130 (0.1, 1, 5, 10, 100 μM; 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 μM, reduces encapsidated HBV DNA by 50% (IC 50 ) and at 18.5 μM by 90% (IC 90 ). AT-130 has no toxic to either HepG2 or Huh-7 cells at concentrations of up to 250 μM. AT-130 (0.005, 0.05, 0.5, 5, 50 μM) 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. AT-130 (2.5, 18.5 μM) 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid

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