Acyclovir
(Synonyms: 阿昔洛韦) 目录号 : GC17186
Acyclovir是一种强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 0.85μM 和 0.86μM。Acyclovir诱导细胞周期紊乱和细胞凋亡。
Cas No.:59277-89-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
Cell lines | Vero cells |
Preparation Method | Vero cells were infected with HSV-1 for 1h and then treated with NPRE (0.1, 0.2, 0.4, 0.6, 0.8mg/mL). The DMSO was used in the control samples and Acyclovir (20µM) was used as positive control. |
Reaction Conditions | 20μM; 3d. |
Applications | Treatment with 20μM Acyclovir showed 100% plaque inhibition. |
| Animal experiment [2]: | |
| Model | Nephrotoxicity Model |
Preparation Method | ICR mice were randomly divided into three groups to receive saline, 150mg/kg Acyclovir, or 600mg/kg Acyclovir once-daily for 9 days. Mice were kept at room temperature and 70±10% humidity, with a light-dark cycle. Food and water were available ad libitum. Acyclovir was administered intraperitoneally (ip) diluted in 20mL/kg of 0.9% sodium chloride injection solution. The saline group received an equal volume of the 0.9% sodium chloride solution. |
Dosage form | 150,600mg/kg; ip; 9d |
Applications | After administration of Acyclovir, levels of serum creatinine and urea nitrogen increased ,mouse kidneys exhibited histopathological changes and reduced expression levels of vascular endothelial growth factor (VEGF) and its receptor VEGFR2. |
References: | |
Acyclovir is a potent oral antiviral drug. Acyclovir has anti-herpetic activity with IC50 values of 0.85 μM and 0.86 μM for HSV-1 and HSV-2, respectively. Acyclovir induces cell cycle disruption and apoptosis[1] [2].
In the plaque reduction assay (PRA) of Vero cells, Acyclovir (20μM; 3d) treatment showed 100% plaque inhibition[1]. Acyclovir (10-100μM; 24-72h) blocks DNA synthesis, thereby arresting the cell cycle at G2/M and S phases and increasing the G1 hypodiploid peak in a dose-dependent manner. Acyclovir (10-100μM; 24-72h) induces apoptosis through activation of caspase-3 and the presence of nuclear DNA fragmentation[2].
Treatment of infected mice with Acyclovir (20mg/kg; po; three times daily; 10d) inhibited the development of skin lesions and led to a dissociation between the DTH response and antibody production [3]. In the Acyclovir-induced nephrotoxicity model, after mice were given Acyclovir (150, 600 mg/kg; ip; 9d), serum creatinine and urea nitrogen levels increased, histopathological changes occurred in the kidneys of mice, and the expression levels of vascular endothelial growth factor (VEGF) and its receptor VEGFR2 were reduced[4].
References:
[1]. Musarra-Pizzo M, Pennisi R, Ben-Amor I, et al. In vitro anti-HSV-1 activity of polyphenol-rich extracts and pure polyphenol compounds derived from pistachios kernels (Pistacia vera L.)[J]. Plants, 2020, 9(2): 267.
[2].Suzuki M, Okuda T, Shiraki K. Synergistic antiviral activity of Acyclovir and vidarabine against herpes simplex virus types 1 and 2 and varicella-zoster virus[J]. Antiviral research, 2006, 72(2): 157-161.
[3]. Benedetti S, Catalani S, Palma F, et al. Acyclovir induces cell cycle perturbation and apoptosis in Jurkat leukemia cells, and enhances chemotherapeutic drug cytotoxicity[J]. Life sciences, 2018, 215: 80-85.
[4].Lu H, Han Y J, Xu J D, et al. Proteomic characterization of acyclovir-induced nephrotoxicity in a mouse model[J]. PLoS One, 2014, 9(7): e103185.
Acyclovir是一种强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 0.85μM 和 0.86μM。Acyclovir诱导细胞周期紊乱和细胞凋亡[1] [2]。
Vero 细胞的噬斑减少试验（PRA）中，Acyclovir（20 μM；3 天）治疗显示 100% 斑块抑制作用[1]。Acyclovir（10-100μM；24-72h）阻断DNA合成，从而将细胞周期停滞在G2/M和S期，并以剂量依赖性方式增加 G1 亚二倍体峰。Acyclovir（10-100μM；24-72h）通过激活caspase-3和存在核 DNA 碎片来诱导细胞凋亡[2]。
Acyclovir（20mg/kg；po；three times daily；10d）治疗感染小鼠可抑制皮肤病变的发展，导致DTH反应与抗体产生之间的解离[3]。在Acyclovir诱导的肾毒性模型中，小鼠给予Acyclovir（150，600mg/kg；ip；9d）后，血清肌酐和尿素氮水平升高，小鼠肾脏出现组织病理学改变，血管内皮生长因子(VEGF)及其受体VEGFR2的表达水平降低[4]。
| Cas No. | 59277-89-3 | SDF | |
| 别名 | 阿昔洛韦 | ||
| 化学名 | 2-amino-9-(2-hydroxyethoxymethyl)-3H-purin-6-one | ||
| Canonical SMILES | C1=NC2=C(N1COCCO)NC(=NC2=O)N | ||
| 分子式 | C8H11N5O3 | 分子量 | 225.21 |
| 溶解度 | ≥ 11.4mg/mL in DMSO | 储存条件 | Store at RT |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.4403 mL | 22.2015 mL | 44.403 mL |
| 5 mM | 0.8881 mL | 4.4403 mL | 8.8806 mL |
| 10 mM | 0.444 mL | 2.2202 mL | 4.4403 mL |
| 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） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 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GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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：取 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 saline，混匀澄清。
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。