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77181-69-2

中文名称 索立夫定
英文名称 sorivudine
CAS 77181-69-2
分子式 C11H13BrN2O6
分子量 349.13
MOL 文件 77181-69-2.mol
更新日期 2024/09/02 21:37:34
77181-69-2 结构式 77181-69-2 结构式

基本信息

中文别名
索立夫定
1-BETA-D-阿拉伯糖呋喃糖基-5-[(1E)-2-溴乙烯基]-2,4(1H,3H)-嘧啶二酮
英文别名
YN-72
BvAraU
D01734
BV-araU
Bravavir
Brovavir
Sorivudin
sorivudine
Bravavir (tn)
Sorivudine (jan/usan/inn)

物理化学性质

熔点182° (Sakata, 1980); mp 195-200° (dec) (Machida, Sakata, 1983)
比旋光度D25 +0.5° (1N NaOH)
密度1.979±0.06 g/cm3(Predicted)
储存条件-20°C储存
溶解度DMSO: 250 mg/mL (716.07 mM)
酸度系数(pKa)8.37±0.10(Predicted)
形态Solid
颜色White to off-white

安全数据

毒性LD50 in mice (mg/kg): ~3300 i.p.; >5000 s.c.; >10000 orally (Machida, Sakata, 1984)

常见问题列表

生物活性
Sorivudine (BV-araU) 是一种口服活性的,合成的嘧啶核苷抗代谢 (pyrimidine nucleoside antimetabolite) 药物。Sorivudine 的抗病毒活性来自某些 DNA 病毒中存在的特定胸苷激酶 (thymidine kinase) 选择性转化为核苷酸,从而反过来会干扰病毒 DNA 合成 (DNA synthesis)。
体外研究

Sorivudine (BV-araU) inhibits strains of HSV-1 and HSV-2 (wild-type strains VR-3 and UW-268) with ID 50 s (50% inhibitory dose) of 0.39 and 0.67 μM, respectively.
Sorivudine has antiviral activity against several viruses including varicella zoster virus, herpes simplex type 1 virus, and Epstein-Barr virus.
Sorivudine (BV-araU) is a pyrimidine nucleoside analog which has in vitro inhibitory activity against varicella zoster virus (VZV) at concentrations of 00001-0.004 mg/ml These concentrations are over 1000-fold lower than those which are required for the inhibition of VZV replication by acyclovir 3 Sorivudine also inhibits HSV-I replication at concentrations ranging from 0.03-0.1 mg/ml.

体内研究

Sorivudine (BV-araU) has been evaluated in the treatment of HSV-l encephalitis when administered orally to mice. At dosages in excess of 12.5 mg/kg, survival of treated mice is prolonged. With doses in excess of 50 mg/kg, a significant decrease in mortality was achieved as we1l. A more relevant model is that of simian varicella virus infection in African green monkeys (Cerophithecus aethiops). In this system, Sorivudine therapy at dosages as low as 20 mg/kg per day given intramuscularly or 100 mg/kg per day administered orally completely protected against viremia and mortality. In the conduct of these studies, there was no evidence of neurotoxicity or abnormalities in hematology or clinical chemistries. Doses as low as 0.2 mg/kg per day were effective; however, breakthrough viremia was noted at lower dosages.

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