Pritelivir mesylate hydrate (BAY 57-1293 mesylate hydrate) 是一种病毒解旋酶-引物酶复合物 (helicase-primase complex) 抑制剂，在体外和单纯疱疹病毒 (HSV) 感染的动物模型中均具有抗病毒活性。Pritelivir mesylate hydrate 对 1 型和 2 型单纯疱疹病毒 (HSV-1和HSV-2) 具有活性，对 HSV1-2 的 IC50为 0.02 μM。
| 生物活性 | Pritelivir mesylate hydrate (BAY 57-1293 mesylate hydrate), an inhibitor of the viralhelicase-primase complex, exhibits antiviral activity in vitro and in animal models of herpes simplex virus (HSV)infection. Pritelivir mesylate hydrate is active against herpes simplex virus types 1 and 2 (HSV-1andHSV-2) with the IC50of 0.02 μM against HSV1-2[1]. |
| IC50& Target[1] | HSV-1 0.02 μM (IC50) | HSV-2 0.02 μM (IC50) |
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体内研究
(In Vivo) | Pritelivir is the first in a class of antiviral agents that inhibit HSV replication by targeting the viral helicase–primase enzyme complex[2].
Pritelivir (0.03-45 mg/kg) significantly increases survival. Pritelivir (0.3-30 mg/kg) reduces mortality against HSV-1, E-377. Pritelivir has potent and resistance-breaking antiviral efficacy with potential for the treatment of potentially life-threatening HSV type 1 and 2 infections, including herpes simplex encephalitis[3].
Combination therapies of Pritelivir at 0.1 or 0.3 mg/kg/dose with Acyclovir (10 mg/kg/dose) are protective when compared to the vehicle treated group against HSV-2, strain MS[3].
| Animal Model: | Female BALB/c mice[3] | | Dosage: | 0.03 to 45 mg/kg | | Administration: | Administered orally, twice daily at approximately 12 h intervals, for 7 days | | Result: | Survival was significantly increased to 80-100% as compared to the vehicle treatment. Even the lowest dose of 0.3 mg/kg was effective in increasing survival to 53%. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
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