Zidovudine
(Synonyms: 叠氮胸苷; Azidothymidine; AZT; ZDV) 目录号 : GC10637
A nucleoside reverse transcriptase inhibitor
Cas No.:30516-87-1
Sample solution is provided at 25 µL, 10mM.
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Zidovudine is an inhibitor of the reverse transcriptase of HIV-1[1].
Zidovudine is the first effective agent for the management of HIV-1 infection and is approved by FDA as a drug for AIDs in 1987. As a nucleoside analogue, zidovudine inhibits the activity of the reverse transcriptase with its triphosphate structure. In the in vitro studies, zidovudine shows strong inhibition of HIV-1 replication and the cytopathic effect of the virus. The addition of 5μM and 10μM zidovudine completely protects TM3 cells (a normal IL-2-dependent helper/inducer T-cell clone) and ATH8 cells against the cytopathic effect of HIV. It exhibits complete inhibition of reverse transcriptase at concentration up to 0.5μM. However, the resistance of zidovudine has been found in vitro and in vivo since 1989 [1, 2].
References:
[1] Mitsuya H, Weinhold K J, Furman P A, et al. 3'-Azido-3'-deoxythymidine (BW A509U): an antiviral agent that inhibits the infectivity and cytopathic effect of human T-lymphotropic virus type III/lymphadenopathy-associated virus in vitro. Proceedings of the National Academy of Sciences, 1985, 82(20): 7096-7100.
[2] McLeod G X, Hammer S M. Zidovudine: five years later. Annals of internal medicine, 1992, 117(6): 487-501.
| Cell experiment [1]: | |
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Cell lines |
SP and 63 cells |
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Preparation method |
The solubility of this compound in DMSO is > 8.4 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
0 ~ 1 mM; 1 hr |
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Applications |
In the pretreated and recently infected SP and 63 cells, Zidovudine exhibited anti-HIV-1 activity, with an ED50 value of 0.001 mM. Moreover, additive effect was observed when Zidovudine was combined with Hydroxychloroquine. Viral replication was reduced to background reverse transcriptase levels. However, Zidovudine did not showed anti-HIV-1 activity towards chronically infected 63HIV and SPH cells. |
| Animal experiment [2]: | |
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Animal models |
Mice |
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Dosage form |
100 mg/kg; p.o.; a single dose |
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Applications |
In mice, the plasma concentration of Zidovudine increased rapidly after administration, reaching 41.69 μg/mL at the 0.75th hr, and followed by a decrease to ~4.64 and 0.45 μg/mL at the 4th and 8th hrs, respectively. The AUC level of Zidovudine was 85.23 ± 5.23 mg*h/mL. The Cmax and tmax values for Zidovudine were 41.69 ± 2.61 μg/mL and 0.75 ± 0.00 hr, respetively. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Chiang G, Sassaroli M, Louie M, Chen H, Stecher VJ, Sperber K. Inhibition of HIV-1 replication by hydroxychloroquine: mechanism of action and comparison with zidovudine. Clin Ther. 1996 Nov-Dec;18(6):1080-92. [2]. Li W, Chang Y, Zhan P, Zhang N, Liu X, Pannecouque C, De Clercq E. Synthesis, in vitro and in vivo release kinetics, and anti-HIV activity of a sustained-release prodrug (mPEG-AZT) of 3'-azido-3'-deoxythymidine (AZT, Zidovudine). ChemMedChem. 2010 Nov 8;5(11):1893-8. | |
| 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 | 0.7484 mL | 3.742 mL | 7.4839 mL |
| 10 mM | 0.3742 mL | 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet