Zidovudine
(Synonyms: 叠氮胸苷; Azidothymidine; AZT; ZDV) 目录号 : GC10637
Zidovudine是一种合成核苷类似物，通过抑制逆转录酶阻断人类免疫缺陷病毒（HIV）的复制。
Cas No.:30516-87-1
Sample solution is provided at 25 µL, 10mM.
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Zidovudine is a synthetic nucleoside analog that blocks replication of the human immunodeficiency virus (HIV) by inhibiting reverse transcriptase[1]. Zidovudine has been used as a model compound to develop a series of related derivatives for viral inhibition studies[2].
In vitro, Zidovudine treatment for 48 hours significantly inhibited HIV-1 activity in primary human fetal astrocytes (PFA) with an EC50 value of 1.311±0.130µM[3]. Treatment with 500μM Zidovudine for 24h induced upregulation of cyclin D1 in HeLa cells and caused a cell arrest in S phase[4]. Treatment of C2C12 cells with 30µM Zidovudine for 8 days resulted in the accumulation of dysfunctional mitochondria and increased reactive oxygen species (ROS) production[5]. Treatment with 1000µM of Zidovudine for 5 weeks resulted in a decrease in checkpoint kinase 1 (Chk1) and checkpoint kinase 2 (Chk2) in NIH 3T3 cells and interference with cell cycle progression[6].
In vivo, Zidovudine treatment (50mg/kg twice daily; i.p.) for 4 weeks significantly resulted in a significant reduction in the levels of various inflammatory markers in the muscles of DMDmdx mouse model[7]. Male OF1 mice were treated with drinking water containing Zidovudine (10mg/kg; p.o.) for 35 days, causing oxidative damage to mitochondrial DNA in the liver of mice [8].
References:
[1] Sperling R. Zidovudine[J]. Infectious diseases in obstetrics and gynecology, 1998, 6(5): 197.
[2] Bianco M C A D, Inacio Leite D, Silva Castelo Branco F, et al. The use of Zidovudine pharmacophore in multi-target-directed ligands for AIDS therapy[J]. Molecules, 2022, 27(23): 8502.
[3] Gray L R, Tachedjian G, Ellett A M, et al. The NRTIs lamivudine, stavudine and zidovudine have reduced HIV-1 inhibitory activity in astrocytes[J]. PloS one, 2013, 8(4): e62196.
[4] Olivero O A, Tejera A M, Fernandez J J, et al. Zidovudine induces S-phase arrest and cell cycle gene expression changes in human cells[J]. Mutagenesis, 2005, 20(2): 139-146.
[5] Lin H, Stankov M V, Hegermann J, et al. Zidovudine-mediated autophagy inhibition enhances mitochondrial toxicity in muscle cells[J]. Antimicrobial Agents and Chemotherapy, 2019, 63(1): 10.1128/aac. 01443-18.
[6] Fang J L, McGarrity L J, Beland F A. Interference of cell cycle progression by zidovudine and lamivudine in NIH 3T3 cells[J]. Mutagenesis, 2009, 24(2): 133-141.
[7] Al-Khalidi R, Panicucci C, Cox P, et al. Zidovudine ameliorates pathology in the mouse model of Duchenne muscular dystrophy via P2RX7 purinoceptor antagonism[J]. Acta Neuropathologica Communications, 2018, 6(1): 27.
[8] de la Asunción J G, del Olmo M L, Sastre J, et al. Zidovudine (AZT) causes an oxidation of mitochondrial DNA in mouse liver[J]. Hepatology, 1999, 29(3): 985-987.
Zidovudine是一种合成核苷类似物，通过抑制逆转录酶阻断人类免疫缺陷病毒（HIV）的复制[1]。Zidovudine作为模型化合物被用于开发一系列相关衍生物以进行病毒抑制研究[2]。
在体外，Zidovudine处理48小时可显著抑制原代人胎儿星形胶质细胞（PFA）中的HIV-1活性，EC50值为1.311±0.130µM[3]。500μM的Zidovudine处理HeLa细胞24小时能诱导细胞周期蛋白D1上调并导致S期阻滞[4]。30µM的Zidovudine处理C2C12细胞8天会导致功能失调线粒体积累和活性氧（ROS）产生增加[5]。1000µM的Zidovudine处理NIH 3T3细胞5周可降低检查点激酶1（Chk1）和检查点激酶2（Chk2）水平，干扰细胞周期进程[6]。
在体内，DMDmdx小鼠模型每日两次腹腔注射Zidovudine（50mg/kg；持续4周）可显著降低肌肉中多种炎症标志物水平[7]。雄性OF1小鼠通过饮用水摄入Zidovudine（10mg/kg；持续35天）会引起肝脏线粒体DNA氧化损伤[8]。
| Cell experiment [1]: | |
Cell lines | HeLa cells |
Preparation Method | HeLa cells (1×106) were cultured in minimum essential medium Eagle supplemented with 10% fetal bovine serum. Zidovudine was dissolved in phosphate-buffered saline and the final concentration was determined by spectrophotometry at 266nm for Zidovudine. Single drug treatments were: 125, 250, and 500μM Zidovudine. After incubating the cells for 24h, the cells were harvested for cell cycle analysis by flow cytometry. |
Reaction Conditions | 125, 250, and 500μM; 24h |
Applications | Zidovudine treatment at 500μM significantly caused an arrest of HeLa cells in S phase. |
| Animal experiment []: | |
Animal models | DMDmdx mouse |
Preparation Method | The DMDmdx mice were raised under standard conditions. Starting from 4 weeks of age, male DMDmdx mice were intraperitoneally injected twice daily for 4 consecutive weeks with 50mg/kg dose of Zidovudine. Age-matched control mice received the same volume of phosphate-buffered saline (pH 7.4). After the treatment, the mice were euthanized by inhalation of carbon dioxide; anterior tibial muscle (TA), gastrocnemius muscle (GC), and cardiac muscle were collected for evaluation. |
Dosage form | 50mg/kg twice daily; for 4 weeks; i.p. |
Applications | Zidovudine treatment significantly resulted in a significant reduction in the mRNA levels of various inflammatory markers in the muscles of mice. |
References: | |
| Cas No. | 30516-87-1 | SDF | |
| 别名 | 叠氮胸苷; Azidothymidine; AZT; ZDV | ||
| 化学名 | 1-[(2R,4S,5S)-4-azido-5-(hydroxymethyl)oxolan-2-yl]-5-methylpyrimidine-2,4-dione | ||
| Canonical SMILES | CC1=CN(C(=O)NC1=O)C2CC(C(O2)CO)N=[N+]=[N-] | ||
| 分子式 | C10H13N5O4 | 分子量 | 267.24 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 10 mg/ml,PBS (pH 7.2): 10 mg/ml | 储存条件 | Store at -20°C |
| 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 | 3.742 mL | 18.7098 mL | 37.4195 mL |
| 5 mM | 748.4 μL | 3.742 mL | 7.4839 mL |
| 10 mM | 374.2 μL | 1.871 mL | 3.742 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。
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Quality Control & SDS
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- Purity: >99.50%
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