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 EC₅₀ of 0.13 μM. 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 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% (IC₅₀) and at 18.5 μM 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 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^[3].
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^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

488.33

C₂₂H₂₂BrN₃O₅

211364-06-6

Room temperature in continental US; may vary elsewhere.

DMSO : 25 mg/mL (51.19 mM; Need ultrasonic)

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请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
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• 1.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.5 mg/mL (5.12 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (5.12 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [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.