AT-130
目录号 : GC61821
An antiviral agent
Cas No.:211364-06-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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)
| 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 |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
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.