AT-130

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AT-130 是 HBV 衣壳组装的有效抑制剂，抑制野生型 HBV 复制，IC50 为 2.4 uM。

AT-130 is a potent inhibitor of HBV capsid assembly, inhibits wild-type HBV replication with IC50 of 2.4 uM; inhibits replication of wild-type and lamivudine-resistant strains of hepatitis B virus in vitro with same sensitivity (rtL180M, rtM204I, and rtL180M + rtM204V); blocks HBV replication at the level of viral RNA packaging, interferes with capsid morphogenesis, shows activity against the main lamivudine- and adefovir-resistant mutants.

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 encapsidated RNA. AT-130 does not affect core protein or nucleocapsid production and the activity of the protein expression vector.

——

AT130

Microbiology/Virology

HBV

HBV

——

——

211364-06-6

488.338

C22H22BrN3O5

>98% (HPLC)

In Vitro:?DMSO : 25 mg/mL (51.19 mM)

O=C(N/C(C(N1CCCCC1)=O)=C(Br)\C2=CC=CC=C2OC)C3=CC=C([N+]([O-])=O)C=C3

(E)-N-(1-bromo-1-(2-methoxyphenyl)-3-oxo-3-(piperidin-1-yl)prop-1-en-2-yl)-4-nitrobenzamide

(-20℃)

With Ice Pack

≥ 2 years