Acyclovir (Synonyms:阿昔洛韦; Aciclovir; Acycloguanosine)
目录号 : KM16462 CAS No. : 59277-89-3 纯度 : 98%

Acyclovir (Aciclovir) 是一种鸟嘌呤类似物和一种具有口服活性的抗病毒剂。Acyclovir 具有抗 HSV-1 (IC50 为 0.85 μM),HSV-2 (IC50 为 0.86 μM) 和水痘带状疱疹病毒的活性。Acyclovir 可被病毒胸苷激酶 (TK) 磷酸化,Acyclovir triphosphate 可干扰病毒 DNA 聚合。Acyclovir 可预防急性白血病的诱导疗法中的细菌感染。

规格 价格 是否有货 数量
50mg
In-stock
100mg
In-stock
500mg
In-stock
1g 询价 In-stock
5g 询价 In-stock

Other Forms of Rapamycin:

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生物活性

Acyclovir (Aciclovir) is a guanosine analogue and an orally active antiviral agent. Acyclovir inhibits HSV-1 (IC50 of 0.85 μM), HSV-2 (IC50 of 0.86 μM) and varicella-zoster virus. Acyclovir can be phosphorylated by viral thymidine kinase (TK), and Acyclovir triphosphate interferes with viral DNA polymerization through competitive inhibition with guanosine triphosphate and obligatory chain termination. Acyclovir prevents bacterial infections during induction therapy for acute leukaemia.

IC50&Target

HSV-1

0.85 μM (IC50)

HSV-2

0.86 μM (IC50)

Bacterial

 

体外研究

Acyclovir (3-100 µM; 24-72 hours; Jurkat, U937, and K562 leukemia cells) treatment shows a dose- and time-dependent reduction of cell viability.
Acyclovir (10-100 µM; 24-72 hours; Jurkat cells) treatment shows a delay/block in S phase and an increase of the sub-G1 peak.
Acyclovir (10-100 µM; 24-72 hours; Jurkat cells) treatment activates caspase-3 and presences nuclear DNA fragmentation, thereby indicating apoptotic cell death.
In HSV-infected cells, HSV thymidine kinase (HSV-TK) specifically phosphorylate Acyclovir to its monophosphate, and this activation confers a high degree of selectivity of the drugs. Thereafter, the monophosphate is further phosphorylated to the diphosphate (Acyclovir -DP) and triphosphate (Acyclovir -TP) by cellular kinases. The triphosphate is the fully activated metabolite that is toxic to the virus.

Cell Viability Assay

Cell Line: Jurkat, U937, and K562 leukemia cells
Concentration: 3 µM, 10 µM, 30 µM, 100 µM
Incubation Time: 24 hours, 48 hours, and 72 hours
Result: Showed a dose- and time-dependent reduction of cell viability.

Cell Cycle Analysis

Cell Line: Jurkat cells
Concentration: 10 µM, 100 µM
Incubation Time: 24 hours, 48 hours, 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.

Apoptosis Analysis

Cell Line: Jurkat cells
Concentration: 10 µM, 100 µM
Incubation Time: 24 hours, 48 hours, and 72 hours
Result: Induced cell apoptosis.
体内研究

Acyclovir (20 mg/kg; oral administration; 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.

Animal Model: Specific-pathogen-free BALB/c mice (7-week-old) infected with HSV-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.
分子式
C8H11N5O3
分子量
225.20
CAS号
59277-89-3
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
溶解性数据
In Vitro: 

DMSO : ≥ 50 mg/mL (222.02 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 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。

临床试验
科研文献
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The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
动物实验计算换算器
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系客服为您提供正确的澄清溶液配方)
+
+
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计算结果:

工作液浓度 mg/ml;

DMSO母液配制方法 mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,

体内配方配制方法μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。

配置后的溶液总体积

1. 首先保证母液是澄清的;
           2. 一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。