Acyclovir (Aciclovir) 是一种有效的口服抗病毒药物。Acyclovir 具有抗疱疹活性，对HSV-1和HSV-2的IC50值分别为 0.85 μM 和 0.86 μM。Acyclovir 诱导细胞周期扰动和凋亡 (apoptosis)。Acyclovir 可预防急性白血病的诱导疗法中的细菌感染。
| 生物活性 | Acyclovir (Aciclovir) is a potent, orally active antiviral agent. Acyclovir has antiherpetic activity withIC50values of 0.85 μM and 0.86 μM forHSV-1andHSV-2, respectively. Acyclovir induces cell cycle perturbation andapoptosis. Acyclovir preventsbacterialinfections during induction therapy for acute leukaemia[1][2][3][4]. |
| IC50& Target[2] | HSV-1 0.85 μM (IC50) | HSV-1 | HSV-2 | HSV-2 0.86 μM (IC50) |
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体外研究
(In Vitro) | Acyclovir (Aciclovir, 3-100 μM; 24-72 hours; Jurkat, U937, and K562 leukemia cells) reduces cell viability in a dose- and time-dependent[1].
Acyclovir (Aciclovir, 10-100 μM; 24-72 hours; Jurkat cells) blocks DNA synthesis, thereby arresting the cell cycle in G2/M and S phases and increasing the sub-G1 hypodiploid peak in a dose-dependent manner[1].
Acyclovir (Aciclovir, 10-100 μM; 24-72 hours; Jurkat cells) induces apoptosis through activates caspase-3 and presences nuclear DNA fragmentation[1].
Cell Viability Assay[1] | Cell Line: | Jurkat, U937 and K562 leukemia cells | | Concentration: | 3, 10, 30 and 100 μM | | Incubation Time: | 24, 48 and 72 hours | | Result: | Showed a dose- and time-dependent reduction of cell viability. |
Apoptosis Analysis[3] | Cell Line: | Jurkat cells | | Concentration: | 10 and 100 μM | | Incubation Time: | 24, 48 and 72 hours | | Result: | Increased of caspase-3 activity and cleavaged the internucleosomal DNA. |
Cell Cycle Analysis[1] | Cell Line: | Jurkat cells | | Concentration: | 10 and 100 μM | | Incubation Time: | 24, 48 and 72 hours | | Result: | Revealed a dose-dependent accumulation of cells in S phase after 24 and 48 h. Showed a dose-dependent increase of the sub-G1 hypodiploid peak after 72 h. |
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体内研究
(In Vivo) | Acyclovir (20 mg/kg; p.o.; three times daily; for 10 days; BALB/c mice) treatment in infected mice suppresses the development of skin lesions and results in a dissociation between DTH response and antibody production[1].
| Animal Model: | Specific-pathogen-free BALB/c mice (7-week-old) infected with HSV-1[1] | | Dosage: | 20 mg/kg | | Administration: | Oral administration; three times daily; for 10 days | | Result: | Suppressed the development of skin lesions and resulted in a dissociation between DTH response and antibody production. |
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| 中文名称 | 阿昔洛韦；阿昔洛维；开糖环鸟苷；羟乙氧甲鸟嘌呤；无环鸟嘌呤核苷；无环鸟嘌呤；无环鸟苷 |
| 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 : ≥ 50 mg/mL(222.02 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 4.4405 mL | 22.2025 mL | 44.4050 mL | | 5 mM | 0.8881 mL | 4.4405 mL | 8.8810 mL | | 10 mM | 0.4440 mL | 2.2202 mL | 4.4405 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 (11.10 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (11.10 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%corn oil Solubility: ≥ 2.5 mg/mL (11.10 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (11.10 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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