索立夫定

索立夫定

中文名称索立夫定
中文同义词索立夫定;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;化合物 T16911
英文名称sorivudine
英文同义词sorivudine;1-(β-D-Arabinofuranosyl)-5-[(E)-2-bromoethenyl]uracil;1-β-D-Arabinofuranosyl-5-[(E)-2-bromovinyl]-1,2,3,4-tetrahydropyrimidine-2,4-dione;Brovavir;BvAraU;BV-araU;YN-72;Bravavir
CAS号77181-69-2
分子式C11H13BrN2O6
分子量349.13
EINECS号
相关类别
Mol文件77181-69-2.mol
结构式索立夫定 结构式

索立夫定 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Store at -20°C
溶解度二甲基亚砜:250 mg/mL(716.07 mM)
酸度系数(pKa)8.37±0.10(Predicted)

索立夫定 用途与合成方法

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)。

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.

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.

安全信息

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

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/01/25HY-123032Sorivudine1 mg552元
2023/03/20HY-123032索立夫定
Sorivudine
77181-69-25mg1450元

索立夫定 上下游产品信息

"索立夫定"相关产品信息
酮康唑 阿糖胸苷 溴夫定 阿糖尿苷 索立夫定
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