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PF-429242 efficiently blocked SKI-1/S1P-mediated processing and subsequent activation of SREBP2 in cell culture and a small animal model. The toxicity profile and pharmacokinetic properties made PF-429242 a promising candidate for a novel anti-arenaviral drug. PF-429242 was able to block the biosynthesis of fusion-active mature GPC of the OW arenaviruses LCMV and LASV and showed potent anti-viral activity against LCMV and LASV in acute infection in cultured cells. These findings suggested the feasibility of using PF-429242 as a novel anti-arenaviral drug. Here we extended these studies and show that PF-429242 is broadly active anti-arenaviral drug that acts in synergy with ribavirin. Moreover, PF-429242 efficiently and rapidly cleared persistent virus from infected cells. Interruption of drug treatment did not result in re-emergence of infection, indicating that PF-429242 treatment resulted in virus extinction.
| Cell Experiment | |
|---|---|
| Cell lines | 293T cells |
| Preparation method | At 5 h posttransfection, the medium was replaced with fresh medium including the indicated concentration of PF-429242. At 36 h posttransfection, cell lysates were prepared (1% NP-40, 50 mM Tris-HCl [pH 8.0], 62.5 mM EDTA, 0.4% sodium deoxycholate) and subjected to sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE), followed by Western blotting (WB). |
| Concentrations | 1, 10, or 30 μM |
| Incubation time | 36 h |
| Animal Experiment | |
|---|---|
| Animal models | A129 mice |
| Formulation | saline |
| Dosages | 2 mg, 1 mg and 0.4 mg per mouse |
| Administration | i.v. |
| Molecular Weight | 409.56 |
| Formula | C25H35N3O2 |
| CAS Number | 947303-87-9 |
| Solubility (25°C) | 10 mM in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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