1. Anti-infection Metabolic Enzyme/Protease
  2. Influenza Virus Drug Metabolite
  3. Oseltamivir acid

Oseltamivir acid  (Synonyms: 奥斯他伟酸; GS 4071; Ro 64-0802; Oseltamivir carboxylate)

目录号: HY-13318 纯度: 99.50%
COA 产品使用指南

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。

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Oseltamivir acid Chemical Structure

Oseltamivir acid Chemical Structure

CAS No. : 187227-45-8

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10 mM * 1 mL in DMSO ¥715
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5 mg ¥650
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10 mg ¥1100
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50 mg ¥3465
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100 mg ¥4950
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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 51 篇科研文献

Proliferation Assay
IF
WB

    Oseltamivir acid purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Jan;97:385-394.  [Abstract]

    The inhibitory effects of OA on M1 protein synthesis and in three different infection protocols. M1 protein expression in H1N1-infected MDCK cells analyzed by Western blot 24 h post infection.

    Oseltamivir acid purchased from MCE. Usage Cited in: Antiviral Res. 2016 May;129:81-92.  [Abstract]

    MDCK cells are infected with K435E or H274Y in the absence of compounds and maintained at 35 °C in agarose with or without 10 nM Oseltamivir or 20 μg/mL D35, respectively.

    Oseltamivir acid purchased from MCE. Usage Cited in: PLoS One. 2016 May 27;11(5):e0156400.  [Abstract]

    Live-cell fluorescence imaging of infected cells of Oseltamivir-resistant virus. MDCK cells are infected with Oseltamivir-resistant 738 and -sensitive 838. After incubation at 37°C for 12 hr, the cells are incubated with BTP3-Neu5Ac with or without Oseltamivir or Zanamivir (each 100 nM for final concentrations) in an SFM at 37°C for 10 min. Fluorescent images of the cells are observed under UV irradiation by using a fluorescence microscope. A scale bar indicates 200 μm.

    Oseltamivir acid purchased from MCE. Usage Cited in: Antiviral Res. 2014 Nov;111:69-77.  [Abstract]

    Plaque formation of different recombinant viruses in the presence of oseltamivir. MDCK cells are infected with recombinant viruses in the absence of Oseltamivir or DS and maintained in agarose overlay medium with 50 nM Oseltamivir or 100 μg/mL DS (DS), or without compounds (None) at 35 °C.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Oseltamivir acid (GS 4071), the active metabolite of Oseltamivir phosphate, is an orally bioavailable, potent and selective inhibitor of influenza virus neuraminidase (IC50=2 nM) with activity against both influenza A and B viruses[1][2].

    IC50 & Target

    IC50: 2 nM (influenza virus neuraminidase)

    体外研究
    (In Vitro)

    Oseltamivir acid 在体外和体内抑制病毒复制。B 型和 A/H1N1 型流感病毒似乎对奥司他韦敏感 (平均 B IC50 值:13 nM;平均 H1N1 IC50 值:1.34 nM),而 A/H1N2 和 A/H3N2 病毒对奥司他韦更敏感 (平均 H3N2 IC50 值:0.67 nM;平均 H1N2 IC50 值:0.9 nM)[3]
    在甲型流感病毒的神经氨酸酶抑制试验中,RWJ-270201 的 IC50 (约 0.34 nM) 与 Oseltamivir acid (0.45 nM) 相当。B 病毒分离株,RWJ-270201 (1.36 nM) 的 IC50 与 Zanamivir (2.7 nM) 相当,低于 Oseltamivir carboxylate (8.5 nM)[4]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    Oseltamivir acid (0.1、1 或 10 mg/kg/天,每日两次,口服强饲法) 对 Vietnam/1203/04 (VN1203/04) 病毒产生剂量依赖性抗病毒作用。10 mg/kg/天的 5 天方案可保护 50% 的小鼠;该处理组的死亡是延迟的,表明处理完成后残留病毒的复制。1 和 10 mg/kg/天的剂量显著降低了器官中的病毒滴度,并分别提供了 60% 和 80% 的存活率[5]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    分子量

    284.35

    Formula

    C14H24N2O4

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    奥斯他伟酸

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : ≥ 230 mg/mL (808.86 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    H2O 中的溶解度 : 100 mg/mL (351.68 mM; 超声助溶)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 3.5168 mL 17.5840 mL 35.1679 mL
    5 mM 0.7034 mL 3.5168 mL 7.0336 mL
    查看完整储备液配制表

    * 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
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    In Vivo:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 5.75 mg/mL (20.22 mM); 澄清溶液

      此方案可获得 ≥ 5.75 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 57.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 5.75 mg/mL (20.22 mM); 澄清溶液

      此方案可获得 ≥ 5.75 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 57.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。

    以下溶解方案,请直接配置工作液。建议现用现配,在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比; 如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶。

    • 方案 一

      请依序添加每种溶剂: PBS

      Solubility: 100 mg/mL (351.68 mM); 澄清溶液; 超声助溶

    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
    您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
    纯度 & 产品资料

    纯度: 99.54%

    参考文献
    Animal Administration
    [3][4]

    Mice[3]
    Female 6-week-old BALB/c mice are anesthetized with isofluorane and intranasally inoculated with 50 μL 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 10 mg/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 50 μL 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 after inoculation. Three mice from each experimental and placebo group are killed, and the lungs and brains are removed. The organs are homogenized and suspended in 1 mL of PBS. The cellular debris is cleared by centrifugation at 2000 g for 5 min. The limit of virus detection is 0.75 log10 EID50. For calculation of the mean, samples with a virus titer <0.75 log10 EID50/mL are assigned a value of 0. Virus titers in each organ are calculated by use of the method of Reed and Muench and are expressed as mean log10 EID50/mL±SE.
    Rats[4]
    Several studies are performed to characterize the pharmacokinetics of Oseltamivir and OC in the plasma, cerebrospinal fluid (CSF), and brain of Sprague-Dawley rats following single-dose bolus administration of Oseltamivir (intravenous [i.v.] and oral) and OC (i.v.). In the i.v. studies, nonfasted adult rats (two groups of 35 animals for each test substance) received a dose of 30 mg/kg body weight of either Oseltamivir or Oseltamivir carboxylate (OC) in aqueous solution with sodium chloride (0.9%; pH 4.0) via slow injection into the tail vein over 20 to 30 s. In both i.v. studies, pharmacokinetic sampling took place at 5 min and at 0.25, 0.5, 1, 2, 4, and 8 h postdose (four or five rats/time point).

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献

    完整储备液配制表

    * 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
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 3.5168 mL 17.5840 mL 35.1679 mL 87.9198 mL
    5 mM 0.7034 mL 3.5168 mL 7.0336 mL 17.5840 mL
    10 mM 0.3517 mL 1.7584 mL 3.5168 mL 8.7920 mL
    15 mM 0.2345 mL 1.1723 mL 2.3445 mL 5.8613 mL
    20 mM 0.1758 mL 0.8792 mL 1.7584 mL 4.3960 mL
    25 mM 0.1407 mL 0.7034 mL 1.4067 mL 3.5168 mL
    30 mM 0.1172 mL 0.5861 mL 1.1723 mL 2.9307 mL
    40 mM 0.0879 mL 0.4396 mL 0.8792 mL 2.1980 mL
    50 mM 0.0703 mL 0.3517 mL 0.7034 mL 1.7584 mL
    60 mM 0.0586 mL 0.2931 mL 0.5861 mL 1.4653 mL
    80 mM 0.0440 mL 0.2198 mL 0.4396 mL 1.0990 mL
    100 mM 0.0352 mL 0.1758 mL 0.3517 mL 0.8792 mL

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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