| 产品描述： | Pimodivir, an influenza A virus polymerases inhibitor via oral, interacts with the viral PB2 subunit. |
| 靶点： |
Influenza Virus;InfluenzaVirus |
| 体外研究： |
Pimodivir is very potent against influenza A strains,and shows potent activity against all influenza A virus strains tested, with an EC50 range of 0.13 to 3.2 nM. |
| 体内研究： |
In mouse influenza model,Pimodivir (1, 3, or 10 mg/kg, bid) provided complete survival. Pimodivir (2, 6, and 20 mg/kg/day, p.o.) completely prevent death in the H1N1pdm virus infection in mice. |
| 细胞实验： |
Pimodivir is dissolved in DMSO.The compound cytotoxicity and efficacy testing is performed in 96-well plates with macrophages at 95% confluence. The compounds are added to the medium, and 30 min later, the cells are infected with virus or non-infected. The cell viability is analyzed with the Cell Titer Glo assay at 24 hpi. The luminescence is read with a PHERAstar FS plate reader. |
| 动物实验： |
The mice, infected intranasally with influenza virus, are given Pimodivir(prepared in 0.5% methylcellulose) twice a day. |
| 参考文献： |
1. Byrn RA, et al. PreClinicalal activity of VX-787, a first-in-class, orally bioavailable inhibitor of the influenza virus polymerase PB2 subunit. Antimicrob Agents Chemother. 2015 Mar;59(3):1569-82. 2. Smee DF, et al. Activities of JNJ63623872 and oseltamivir against influenza A H1N1pdm and H3N2 virus infections in mice. Antiviral Res. 2016 Dec;136:45-50. 3. Fu Y, et al. JNJ872 inhibits influenza A virus replication without altering cellular antiviral responses. Antiviral Res. 2016 Sep;133:23-31. 4. Boyd MJ, et al. Isosteric replacements of the carboxylic acid of drug candidate VX-787: Effect of charge on antiviral potency and kinase activity of azaindole-based influenza PB2 inhibitors. Bioorg Med Chem Lett. 2015 May 1;25(9):11990-4. |
| 溶解性： |
soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.504 ml |
12.519 ml |
25.038 ml |
| 5 mM |
0.501 ml |
2.504 ml |
5.008 ml |
| 10 mM |
0.25 ml |
1.252 ml |
2.504 ml |
| 50 mM |
0.05 ml |
0.25 ml |
0.501 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京