奥斯他伟酸

奥斯他伟酸

中文名称奥斯他伟酸
中文同义词奥斯他伟酸;奥斯他伟酸(奥司他韦羧酸);奥司他韦羧酸;奥司他韦酸;奥塞米韦酸;奥司他韦酒石酸盐;奥司他韦10;奥司他韦杂质C(EP)
英文名称OSELTAMIVIR ACID
英文同义词Oseltamivir acid, >=98%;Oseltamivir EP Impurity C;Oseltamivir carboxylate (OC),Metabolite of oseltamivir;(3R,4R,5S)-4-acetamido-5-amino-3-(pentan-3-yloxy)cyclohex-1-enecarboxylic acid;(3R,4R,5S)-4-Acetamido-5-amino-3-(1-ethylpropoxy)-1-cyclohex-ene-1-carboxylic acid;1-Cyclohexene-1-carboxylic acid, 4-(acetylamino)-5-amino-3-(1-ethylpropoxy)-, (3R,4R,5S)-;204255-11-8 (Monophospate salt);Aids095377
CAS号187227-45-8
分子式C14H24N2O4
分子量284.35
EINECS号
相关类别杂质对照品;奥司他韦;对照品-杂质对照品;医药原料;Various Metabolites and Impurities;Metabolites;Amines;Intermediates & Fine Chemicals;Metabolites & Impurities;Pharmaceuticals
Mol文件187227-45-8.mol
结构式奥斯他伟酸 结构式

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
形态固体
酸度系数(pKa)4.13±0.60(Predicted)
颜色白色至米白色
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

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。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。

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.

安全信息

海关编码9999999999

MSDS信息

奥斯他伟酸 上下游产品信息

"奥斯他伟酸"相关产品信息
磷酸奥司他韦 (3R,4R,5S)-4-(乙酰氨基)-5-氨基-3-(1-甲基丙氧基)-1-环己烯-1-羧酸乙酯 奥司他韦杂质G OseltaMivirIMpurityD 磷酸奥司他韦EP杂质E 5-(乙酰氨基)-4-氨基-3-(1-乙基丙氧基)-1-环己烯-1-羧酸 奥司他韦杂质 (3S,4S,5R)-4-(乙酰氨基)-5-氨基-3-(1-乙基丙氧基)-1-环己烯-1-羧酸乙酯磷酸盐 奥司他韦杂质 奥司他韦杂质 奥司他韦
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