奥斯他伟酸
- CAS号:187227-45-8
- 英文名:OSELTAMIVIR ACID
- 中文名:奥斯他伟酸
- CBNumber:CB6501589
- 分子式:C14H24N2O4
- 分子量:284.35
- MOL File:187227-45-8.mol
- 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 :Keep in dark place,Sealed in dry,2-8°C
- 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
- 形态 :Solid
- 酸度系数(pKa) :4.13±0.60(Predicted)
- 颜色 :White to off-white
- EPA化学物质信息 :1-Cyclohexene-1-carboxylic acid, 4-(acetylamino)-5-amino-3-(1-ethylpropoxy)-, (3R,4R,5S)- (187227-45-8)
- 海关编码 :9999999999
奥斯他伟酸性质、用途与生产工艺
- 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。
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靶点
IC50: 2 nM (influenza virus neuraminidase)
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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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