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Fialuridine
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Fialuridine图片
CAS NO:69123-98-4
规格:98%
分子量:372.1
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议

产品介绍
nucleoside analog with antiviral activity
CAS:69123-98-4
分子式:C9H10FIN2O5
分子量:372.1
纯度:98%
存储:Store at -20°C

Background:

Ki: 0.14 and 0.95 μM for herpes simplex virus types 1 and 2, respectively


Fialuridine is a nucleoside analog with antiviral activity.


Nucleoside analogues mimic physiological nucleosides in terms of uptake and metabolism and are incorporated into newly synthesized DNA resulting in synthesis inhibition and chain termination.


In vitro: Previous in-vitro data showed that 1-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl)-5-ethyluracil (FEAU) had activity against herpes simplex virus types 1 and 2 comparable to that of 1-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl)-5-methyluracil (FMAU), fialuridine (FIAU), and acyclovir (ACV). The cellular toxicity of FEAU was found to be much lower than that of FIAU. Biochemical experiments indicated that FEAU had similar affinity toward thymidine kinases encoded by HSV 1 and 2 and a much lower affinity for cellular thymidine kinase than thymidine [1].


In vivo: The in-vivo antiviral efficiency of FEAU was compared with that of FIAU and ACV by using the herpes encephalitis mode. Moreover, ACV and FEAU could significantly increase the number of survivors at doses of 50 and 100 mg/kg per day, respectively, and FIAU showed significant activity at 25 mg/kg per day in the animal model [1].


Clinical trial: In patients with chronic hepatitis B, fialuridine treatment induced a severe toxic reaction demonstrated by hepatic failure, lactic acidosis, pancreatitis, neuropathy, as well as myopathy. Such toxic reaction was probably caused by widespread mitochondrial damage and [2].


参考文献:
[1] Mansuri, M. M.,Ghazzouli, I.,Chen, M.S., et al. 1-(2-Deoxy-2-fluoro-β-D-arabinofuranosyl)-5-ethyluracil. A highly selective antiherpes simplex agent. Journal of Medicinal Chemistry 30(5), 867-871 (1987).
[2] McKenzie R et al. Hepatic failure and lactic acidosis due to fialuridine (FIAU), an investigational nucleoside analogue for chronic hepatitis B. N Engl J Med. 1995 Oct 26;333(17):1099-105.