| Description | Pimodivir (VX-787), an influenza A virus polymerases inhibitor via oral, interacts with the viral PB2 subunit. |
| In vitro | 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. |
| In vivo | 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. |
| Cell experiments | 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. |
| Animal experiments | The mice, infected intranasally with influenza virus, are given Pimodivir(prepared in 0.5% methylcellulose) twice a day. |
| Synonyms | VX-787 |
| molecular weight | 399.39 |
| Molecular formula | C20H19F2N5O2 |
| CAS | 1629869-44-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 60 mg/mL (150.23 mM) |
| References | 1. 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. 2. Fu Y, et al. JNJ872 inhibits influenza A virus replication without altering cellular antiviral responses. Antiviral Res. 2016 Sep;133:23-31. 3. 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. 4. 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. |