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索立夫定

索立夫定

中文名稱索立夫定
中文同義詞索立夫定;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;索里呋啶;5-((E)-2-溴乙烯基)-1-((2R,3S,4S,5R)-3,4-二羥基-5-(羥甲基)四氫呋喃-2-基)嘧啶-2,4(1H,3H)-二酮;索利夫定
英文名稱sorivudine
英文同義詞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號77181-69-2
分子式C11H13BrN2O6
分子量349.13
EINECS號
相關類別
Mol文件77181-69-2.mol
結構式索立夫定 結構式

索立夫定 性質

熔點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)
儲存條件Store at -20°C
溶解度二甲基亞砜:250 mg/mL(716.07 mM)
形態(tài)固體
酸度系數(shù)(pKa)8.37±0.10(Predicted)
顏色白色至米白色

索立夫定 用途與合成方法

Sorivudine (BV-araU) 是一種口服活性的,合成的嘧啶核苷抗代謝 (pyrimidine nucleoside antimetabolite) 藥物。Sorivudine 的抗病毒活性來自某些 DNA 病毒中存在的特定胸苷激酶 (thymidine kinase) 選擇性轉化為核苷酸,從而反過來會干擾病毒 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

更新日期產品編號產品名稱CAS號包裝價格
2026/06/05HY-123032索立夫定
Sorivudine
77181-69-21 mg552元
2026/06/05HY-123032索立夫定
Sorivudine
77181-69-25mg1650元

索立夫定 上下游產品信息

"索立夫定"相關產品信息
酮康唑 阿糖胸苷 溴夫定 阿糖尿苷 索立夫定
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