product name Zidovudine
Description: Zidovudine (also known as ZDV, Azidothymidine; Retrovir; Zidovudinum, NSC 602670) is a nucleoside analogue reverse transcriptase inhibitor, used to treat HIV. 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.
References: Clin Ther. 1996;18(6):1080-92; J Med Virol. 1999 Jun;58(2):165-73; Biochim Biophys Acta. 1996;1316(1):51-9.
267.24
Formula
C10H13N5O4
CAS No.
30516-87-1
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 53 mg/mL (198.3 mM)
Water: 53 mg/mL (198.3 mM)
Ethanol:
Solubility (In vivo)
18 mg/mL (67.4 mM)
Synonyms
Azidothymidine, NSC 602670, Retrovir; Zidovudinum
other peoduct :
| In Vitro |
In vitro activity: Zidovudine pretreatment has potent anti-HIV-1 activity in the newly infected T and monocytic cells but not in chronically infected cells. Inhibition of reverse transcription by Zidovudine decreases p24 antigen levels modestly, decreased HIV-1 gag by 19-fold, and inhibits detection of 2-LTR HIV-1 DNA. Zidovudine and dideoxynucleosides deplete wild-type mitochondrial DNA levels and increase deletedmitochondrial DNA levels in cultured Kearns-Sayre syndrome fibroblasts. Zidovudine (AZT, 0.1-50 mM) has a concentration dependent suppressive effect on the growth of granulocyte-monocyte colony forming unit (CFU-GM) derived colonies. Zidovudine exposure also induces a concentration dependent suppressive effect (35-90%) on GM-CSF receptor type alpha (GM-CSFR alpha) gene expression. Zidovudine causes a much lower decrease (15-22%) on the IL-3 receptor type alpha (IL-3R alpha) message level, and has an insignificant effect on glyceraldehyde 3-phosphate dehydrogenase (GAPDH) and c-myc message levels. Zidovudine causes a concentration-dependent inhibition in the levels of the mRNA of Epo receptors and c-fos, whereas the level of c-myc mRNA is unaffected. Zidovudine also inhibits protein kinase C (PKC) activity in a concentration- and time-dependent manner, causing 50% inhibition at 10 mM within 3 hours. Zidovudine-induced down-regulation of Epo receptors and c-fos expression coupled with inhibition of Epo receptor-mediated signal transduction through PKC are significant contributory factors to AZT-induced erythroid toxicity. Kinase Assay: Cell Assay: |
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| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | Clin Ther. 1996 Nov-Dec;18(6):1080-92; J Med Virol. 1999 Jun;58(2):165-73; Biochim Biophys Acta. 1996 May 24;1316(1):51-9. |
