S83758 |
Pimodivir |
源叶(MedMol) | 99% |
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- 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
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)