CAS NO: | 133525-01-6 |
包装 | 价格(元) |
1mg | 电议 |
5mg | 电议 |
10mg | 电议 |
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 465.4 |
Cas No. | 133525-01-6 |
Formula | C16H20N5O10·Na |
Synonyms | AZT glucuronide,Zidovudine glucuronide |
Solubility | ≤0.5mg/ml in DMSO |
Chemical Name | 3'-azido-3'-deoxy-5'-O-β-D-glucopyranuronosyl-thymidine, monosodium salt |
Canonical SMILES | O=C([O-])[C@@H](O1)[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1OC[C@@H]2[C@@H](N=[N+]=[N-])C[C@H](N3C=C(C)C(NC3=O)=O)O2.[Na+] |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。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。 |
3'-Azido-3'-deoxythymidine β-D-glucuronide is the metabolite of zidovudine, a nucleoside reverse transcriptase inhibitor.
Zidovudine, an antiretroviral medication used to prevent and treat HIV, is recommended for use with other antiretroviral and may be also used to prevent mother to child spread during birth or after a needlestick injury or other potential exposure.
In vitro: 3'-Azido-3'-deoxythymidine β-D-glucuronide is a metabolite of zidovudine, formed by direct conjugation by UDP-glucuronosyltransferase 2B7. The azido group of both zidovudine and 3'-azido-3'-deoxythymidine β-D-glucuronide could be reduced to an amino group by cytochrome CYP3A, CYP2A6, or CYP2B1, forming 3’-amino-3’-deoxythymidine (AMT) and AMT glucuronide, respectively [1].
In vivo: Animal study found that zidovudine-treated rats had higher systolic blood pressure, greater heart weight and greater interventricular septum thickness. Electron microscopy revealed mitochondrial swelling in myocardiocytes in zidovudine-treated rats. Reduced response to contractile stimuli and enhanced relaxation in response to charbacol were observed in the aortic rings of zidovudine-treated rats. The aortic myocytes of zidovudine-treated rats contained apparently unaffected ultrastructural features, but light microscopy suggested their marked enlargement [2].
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Walsky, R. L.,Bauman, J.N.,Bourcier, K., et al. Optimized assays for human UDP-glucuronosyltransferase (UGT) activities: altered alamethicin concentration and utility to screen for UGT inhibitors. Drug Metabolism and Disposition 40(5), 1051-1065 (2012).
[2] Ruga E, Bova S, Nussdorfer G, Mazzocchi G, Rebuffat P, Milanesi O, Cargnelli G. Zidovudine-induced alterations in the heart and vascular smooth muscle of the rat. Cardiovasc Res. 2003 Oct 15;60(1):147-55.