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奥斯他伟酸  ≥98%

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包装规格：5mg 10mg 50mg 250mg in glass bottle
溶解性：溶于DMSO（≥ 230 mg/mL)
产品描述：基本信息 产品编号：O10192 产品名称：Oseltamivir acid CAS: 187227-45-8   储存条件 粉末 -20℃ 四年 分子式： C14H24N2O4 溶于液体 -80℃ 两年 分子量 284.35 -20℃ 一个月 化学名：  (3R,4R,5S)-4-acetamido-5-amino-3-pentan-3-yloxycyclohexene-1-carboxylic acid   Solubility (25°C)   体外 DMSO ≥230mg/mL (808.86mM) Ethanol   Water 100mg/mL (351.68mM; Need ultrasonic) 体内 现配现用   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 3.5168mL 17.5840mL 35.1679mL 5mM 0.7034mL 3.5168mL 7.0336mL 10mM 0.3517mL 1.7584mL 3.5168mL   生物活性 产品描述 Oseltamivir phosphate 的活性代谢产物, 是流感病毒神经氨酸酶 (IC50=2nM) 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 influenza virus neuraminidase IC50: 2nM   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 IC50 value: 13nM; mean H1N1 IC50 value: 1.34nM), while A/H1N2 and A/H3N2 viruses are more sensitive to Oseltamivir (mean H3N2 IC50 value: 0.67nM; mean H1N2 IC50 value: 0.9nM).In neuraminidases inhibition assays with influenza A viruses, the IC50 of RWJ-270201 (approximately 0.34nM) is comparable to that of Oseltamivir carboxylate (0.45nM) For influenza B virus isolates, the IC50 of RWJ-270201 (1.36nM) is comparable to that of Zanamivir (2.7nM) and less than that of Oseltamivir carboxylate (8.5nM).   体内研究 Oseltamivir (0.1, 1, or 10mg/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 1,000mg/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 (AUC0-8 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 (AUC0-8 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.   推荐实验方法(仅供参考) 动物实验:   Animal Administration Mice Female 6-week-old BALB/c mice are anesthetized with isofluorane and intranasally inoculated with 50μL of 10-fold serial dilutions of VN1203/04 virus in PBS. The mouse lethal dose (MLD50) is calculated after a 16-day observation period.Oseltamivir is administered by oral gavage twice daily for 5 or 8 days to groups of 10 mice at dosages of 0.1, 1, and 10mg/kg/day. Control (infected but untreated) mice received sterile PBS (placebo) on the same schedule. Four hours after the first dose of Oseltamivir, the mice are inoculated intranasally with 5 MLD50 of VN1203/04 virus in 50μL of PBS. Survival and weight change are observed for 24 days. Virus titers in the mouse organs are determined on days 3, 6, and 9 afte
保存条件：-20℃

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