Pritelivir (AIC316) 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 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 (AIC316), an inhibitor of the viralhelicase-primase complex, exhibits antiviral activity in vitro and in animal models of herpes simplex virus (HSV)infection. Pritelivir 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 | 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 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : ≥ 33 mg/mL(81.99 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 2.4845 mL | 12.4227 mL | 24.8453 mL | | 5 mM | 0.4969 mL | 2.4845 mL | 4.9691 mL | | 10 mM | 0.2485 mL | 1.2423 mL | 2.4845 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (6.21 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.21 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (6.21 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.21 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (6.21 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.21 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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