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187227-45-8

中文名称 奥斯他伟酸
英文名称 OSELTAMIVIR ACID
CAS 187227-45-8
分子式 C14H24N2O4
分子量 284.354
MOL 文件 187227-45-8.mol
更新日期 2024/03/28 16:40:33
187227-45-8 结构式 187227-45-8 结构式

基本信息

中文别名
奥斯他伟酸
奥塞米韦酸
奥司他韦酸
奥司他韦羧酸
奥司他韦酒石酸盐
奥斯他伟酸(奥司他韦羧酸)
英文别名
Gs4071
Gs-4071
Gs 4071
Aids095377
Aids-095377
Oseltamivir impurity C
Oseltamivir carboxylate
Oseltamivir acid, >=98%
Oseltamivir EP Impurity C
OseltaMivir carboxylic acid

物理化学性质

熔点183-185°C
沸点508.7±50.0 °C(Predicted)
密度1.15±0.1 g/cm3(Predicted)
储存条件-20°C 冰箱,在惰性气氛下稳定
溶解度≥14.2 mg/mL in DMSO; ≥46.1 mg/mL in H2O with gentle warming; ≥97 mg/mL in EtOH with gentle warming
酸度系数(pKa)4.13±0.60(Predicted)
形态neat

安全数据

危险性符号(GHS)
GHS07
警示词警告
危险性描述H302-H315-H319-H335

常见问题列表

产品描述
奥司他韦酸是制备奥司他韦的中间体。磷酸奥司他韦是由瑞士罗氏公司研发推出,磷酸奥司他韦具有很强的抑制神经氨酸酶的活性,对A、B型流感病毒均有效。
生物活性
Oseltamivir acid (GS 4071),Oseltamivir phosphate 的活性代谢产物, 是流感病毒神经氨酸酶 (IC50=2 nM) 的口服生物有效的,选择性的抑制剂,对流感病毒 A 和 B 都有活性。
靶点

IC50: 2 nM (influenza virus neuraminidase)

体外研究

Oseltamivir acid inhibits virus replication in vitro and in vivo. Influenza B and A/H1N1 viruses appeare to be sensitive to Oseltamivir (mean B IC 50 value: 13 nM; mean H1N1 IC 50 value: 1.34 nM), while A/H1N2 and A/H3N2 viruses are more sensitive to Oseltamivir (mean H3N2 IC 50 value: 0.67 nM; mean H1N2 IC 50 value: 0.9 nM).
In neuraminidases inhibition assays with influenza A viruses, the IC 50 of RWJ-270201 (approximately 0.34 nM) is comparable to that of Oseltamivir carboxylate (0.45 nM) For influenza B virus isolates, the IC 50 of RWJ-270201 (1.36 nM) is comparable to that of Zanamivir (2.7 nM) and less than that of Oseltamivir carboxylate (8.5 nM).

体内研究

Oseltamivir (0.1, 1, or 10 mg/kg/day, twice daily by oral gavage) produces a dose-dependent antiviral effect against Vietnam/1203/04 (VN1203/04) virus. The 5-day regimen at 10 mg/kg/day protects 50% of mice; deaths in this treatment group are delayed and indicated the replication of residual virus after the completion of treatment. Eight-day regimens improved Oseltamivir efficacy, and dosages of 1 and 10 mg/kg/day significantly reduced virus titers in organs and provided 60% and 80% survival rates, respectively.
In the pharmacokinetic study, after the oral administration of 1,000 mg/kg Oseltamivir, peak plasma concentrations are reached at 2 h postdose for Oseltamivir and 8 h for Oseltamivir carboxylate (OC). Rats are exposed to Oseltamivir over the whole sampling interval and had a ~2.7-fold-higher rate of exposure to OC than Oseltamivir. In CSF, peak concentrations are reached at 2 h postdose for Oseltamivir and 6 h for OC. CSF/plasma exposure ratios (AUC 0-8 h ) are ~0.07 for Oseltamivir and 0.007 for OC. In perfused brain samples, peak concentrations are reached at 8 h postdose for Oseltamivir and 6 h for OC. Brain/plasma exposure ratios (AUC 0-8 h ) of ~0.12 for Oseltamivir and 0.01 for OC are recorded. Corresponding CSF/brain exposure ratios ranged between ~0.55 and 0.64 for both analytes. A further group of animals that received a single oral administration of Oseltamivir at a lower dose produced similar results.

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