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AT-130 Sale

目录号 : GC61821

An antiviral agent

AT-130 Chemical Structure

Cas No.:211364-06-6

规格 价格 库存 购买数量
5 mg
¥1,800.00
现货
10 mg
¥3,420.00
现货
25 mg
¥5,400.00
现货
50 mg
¥9,450.00
现货
100 mg
¥14,040.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

AT-130 is an antiviral agent.1,2 It is a non-nucleoside inhibitor of hepatitis B virus (HBV) replication in wild-type and rtL180M, rtM204I, and rtL180M + rtL204V lamivudine-resistant strains of HBV (IC50s = 2.4, 1.6, 5.1, and 1.3 ?M, respectively).2 AT-130 inhibits viral DNA synthesis in HBV-infected HepAD38 cells (EC50 = 0.13 ?M) and reduces the amount of encapsidated RNA in HBV-infected HepG2 cells.2,3

1.Perni, R.B., Conway, S.C., Ladner, S.K., et al.Phenylpropenamide derivatives as inhibitors of hepatitis B virus replicationBioorg. Med. Chem. Lett.10(23)2687-2690(2000) 2.Delaney, W.E., IV, Edwards, R., Colledge, D., et al.Phenylpropenamide derivatives AT-61 and AT-130 inhibit replication of wild-type and lamivudine-resistant strains of hepatitis B virus in vitroAntimicrob. Agents Chemother.46(9)3057-3060(2002) 3.Feld, J.J., Colledge, D., Sozzi, V., et al.The phenylpropenamide derivative AT-130 blocks HBV replication at the level of viral RNA packagingAntiviral Res.76(2)168-177(2007)

Chemical Properties

Cas No. 211364-06-6 SDF
Canonical SMILES O=C(N/C(C(N1CCCCC1)=O)=C(Br)\C2=CC=CC=C2OC)C3=CC=C([N+]([O-])=O)C=C3
分子式 C22H22BrN3O5 分子量 488.33
溶解度 DMSO : 25 mg/mL (51.19 mM) 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 2.0478 mL 10.239 mL 20.478 mL
5 mM 0.4096 mL 2.0478 mL 4.0956 mL
10 mM 0.2048 mL 1.0239 mL 2.0478 mL
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Research Update

The phenylpropenamide derivative AT-130 blocks HBV replication at the level of viral RNA packaging

Antiviral Res 2007 Nov;76(2):168-77.PMID:17709147DOI:10.1016/j.antiviral.2007.06.014.

Nucleos(t)ide analogue antiviral therapy for chronic hepatitis B has proven to be effective in the short term but the frequent development of resistance limits its clinical utility. Agents targeting other stages of viral replication are needed in order to develop improved combination therapies. The phenylpropenamide derivatives AT-61 and AT-130 have been shown to inhibit HBV replication in vitro, but the mechanism of action of these compounds remains undefined. The aim of this study was to determine the mechanism of action of AT-130, a non-nucleoside inhibitor of HBV in several in vitro models of replication. These studies found that AT-130 inhibited HBV DNA replication in hepatoma cells but had no effect on viral DNA polymerase activity or core protein translation. Total HBV RNA production was also unaffected in the presence of the drug whilst the amount of encapsidated RNA was significantly reduced, thereby inhibiting subsequent viral reverse transcription. These studies have established that the inhibition of HBV genome replication by a non-nucleoside analogue acting at the level of viral encapsidation and packaging is a potentially useful strategy for future therapeutic drug development in the management of chronic hepatitis B.

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.PMID:12183271DOI:10.1128/AAC.46.9.3057-3060.2002.

The phenylpropenamide derivatives AT-61 and AT-130 are nonnucleoside analogue inhibitors of hepatitis B virus (HBV) replication. They inhibited the replication of wild-type HBV with 50% inhibitory concentrations of 21.2 +/- 9.5 and 2.40 +/- 0.92 micro M, respectively, compared to 0.064 +/- 0.020 micro M lamivudine. There were no significant differences in sensitivity between wild-type and nucleoside analogue-resistant (rtL180M, rtM204I, and rtL180M + rtM204V) HBV.