中文名称: 奥斯他伟酸
英文名称: Oseltamivir acid
CAS No: 187227-45-8
分子式: C14H24N2O4
分子量: 284.35
O10192 奥斯他伟酸 ≥98% (psaitong)
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℃
UN码:
HazardClass:
危害声明:
安全说明:
搜索质检报告(COA)
参考文献 & 客户发表文献

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

  • =
    *
    *
    *选择对应的单位 *空出希望得到的变量,填写另外两个变量

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 )

  • * = *

连续稀释计算器方程

  • 连续稀释

  • 初始浓度:
  • 稀释倍数:
  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):