AT-130
目录号: PL01019 纯度: ≥98%
CAS No. :211364-06-6
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中文名称
AT-130
英文名称
AT-130
英文别名
Benzamide,N-[(1E)-2-bromo-2-(2-methoxyphenyl)-1-(1-piperidinylcarbonyl)ethenyl]-4-nitro-;AT-130;(E)-N-(1-bromo-1-(2-methoxyphenyl)-3-oxo-3-(piperidin-1-yl)prop-1-en-2-yl)-4-nitrobenzamide;N-[(1e)-1-Bromo-1-(2-Methoxyphenyl)-3-Oxo-3-(Piperidin-1-Yl)prop-1-En-2-Yl]-4-Nitrobenzamide;at130;N-[(E)-1-bromo-1-(2-methoxyphenyl)-3-oxo-3-piperidin-1-ylprop-1-en-2-yl]-4-nitrobenzamide;N-[(E)-2-Bromo-2-(2-methoxyphenyl)-1-(piperidine-1-carbonyl)vinyl]-4-nitro-benzamide;N-[(E)-alpha-(Piperidinocarbonyl)-beta-bro
Cas No.
211364-06-6
分子式
C22H22BrN3O5
分子量
488.33
包装储存
Powder -20°C 3 years;In solvent -80°C 6 months
产品详情
AT-130 是一种苯基丙烯酰胺衍生物,是一种有效的乙型肝炎病毒 (HBV) 复制的非核苷抑制剂。AT-130 抑制病毒 DNA 的合成,EC50 为 0.13 μM。AT-130 可以抑制野生型和突变型 HBV。AT-130 在肝癌细胞中具有抗 HBV 活性。
生物活性
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.
性状
Solid
体外研究(In Vitro)
AT-130 inhibits Wt HBV (IC50=2.4 μM), rtL180M HBV (IC50=9.8 μM), rtM204I HBV (IC50=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% (IC50) and at 18.5 μM by 90% (IC90).
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 encap
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;In solvent -80°C 6 months
ClinicalTrial
参考文献
[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.
溶解度数据
In Vitro: DMSO : 25 mg/mL (51.19 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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