奥斯他伟酸
奥斯他伟酸 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 | Keep in dark place,Sealed in dry,2-8°C |
| 溶解度 | DMSO 中≥14.2 mg/mL；温和加热时，水中≥46.1 mg/mL；温和加热时，EtOH 中浓度≥97 mg/mL |
| 酸度系数(pKa) | 4.13±0.60(Predicted) |
| 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) |
奥斯他伟酸 用途与合成方法
IC50: 2 nM (influenza virus neuraminidase)
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).
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.
