Zidovudine
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Zidovudine是一种HIV-1逆转录酶的抑制剂[1].
Zidovudine是第一种处理HIV-1感染的有效制剂,并在1987年被FDA批准为AIDs药物.作为核苷类似物,zidovudine可用其三磷酸结构抑制逆转录酶活性.在体外研究中,zidovudine可强力抑制HIV-1复制和病毒的细胞病变作用.添加5 μM和10 μM的zidovudine可完全保护TM3细胞(一种正常的IL-2依赖的辅助/诱导T细胞克隆)和ATH8细胞免受HIV的细胞病变作用.该物质在高达0.5 μM浓度时可完全抑制逆转录酶.但是,1989年起zidovudine的体外和体内耐受性被发现[1,2].
参考文献:
[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.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 267.24 |
Cas No. | 30516-87-1 |
Formula | C10H13N5O4 |
Solubility | ≥17.6 mg/mL in H2O with gentle warming and ultrasonic; ≥26.5 mg/mL in EtOH with gentle warming; ≥8.35 mg/mL in DMSO |
Chemical Name | 1-[(2R,4S,5S)-4-azido-5-(hydroxymethyl)oxolan-2-yl]-5-methylpyrimidine-2,4-dione |
SDF | Download SDF |
Canonical SMILES | CC1=CN(C(=O)NC1=O)C2CC(C(O2)CO)N=[N+]=[N-] |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1]: | |
细胞系 |
SP细胞和63细胞 |
制备方法 |
在DMSO中的溶解度大于8.4 mg/mL。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。 |
反应条件 |
0 ~ 1 mM;1小时 |
实验结果 |
在最近受感染的SP细胞和63细胞中,使用Zidovudine进行预处理有效对抗HIV-1病毒,其ED50值为0.001 mM。此外,Zidovudine与Hydroxychloroquine联合用药具有协同作用。病毒复制降低到背景逆转录酶水平。然而,Zidovudine对慢性感染的63HIV和SPH细胞没有显示出抗HIV-1活性 |
动物实验 [2]: | |
动物模型 |
小鼠 |
给药剂量 |
100 mg/kg;口服给药;单次给药 |
实验结果 |
在小鼠中,Zidovudine血浆浓度于给药后迅速增加。在第0.75小时,其血浆浓度达41.69 μg/mL。在第4和第8小时,相应的血浆浓度分别降至~4.64 μg/mL和0.45 μg/mL。Zidovudine的AUC水平为85.23 ± 5.23 mg*h/mL。Zidovudine的Cmax和tmax值分别为41.69 ± 2.61 μg/mL和0.75 ± 0.00小时。 |
注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。 |
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. |
质量控制和MSDS
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