中文名称: | 奥斯他伟酸 | ||||
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英文名称: | Oseltamivir acid | ||||
别名: | 奥司他韦酸;奥塞米韦酸 GS 4071; Ro 64-0802; Oseltamivir carboxylate | ||||
CAS No: | 187227-45-8 | 分子式: | C14H24N2O4 | 分子量: | 284.35 |
CAS No: | 187227-45-8 | ||||
分子式: | C14H24N2O4 | ||||
分子量: | 284.35 |
基本信息
产品编号:O10192 |
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产品名称:Oseltamivir acid |
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CAS: |
187227-45-8 |
储存条件 |
粉末 |
-20℃ |
四年 |
分子式: |
溶于液体 |
-80℃ |
两年 |
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分子量 |
284.35 |
-20℃ |
一个月 |
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化学名: |
(3R,4R,5S)-4-acetamido-5-amino-3-pentan-3-yloxycyclohexene-1-carboxylic acid |
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Solubility (25°C) |
体外 |
DMSO |
≥230mg/mL (808.86mM) |
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Ethanol |
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Water |
100mg/mL (351.68mM; Need ultrasonic) |
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体内 |
现配现用 |
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<1mg/ml表示微溶或不溶。 |
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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。 |
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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: |
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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 |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )