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Oseltamivir acid

Oseltamivir acid

产品编号 T5186   CAS 187227-45-8
别名: GS 4071, oseltamivir carboxylate, 奥斯他伟酸, Ro 64-0802

Oseltamivir acid (GS 4071) 是Oseltamivir phosphate 的活性代谢产物,是一种有效的流感病毒神经氨酸酶抑制剂和 GS4071 的前药。

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Oseltamivir acid Chemical Structure
Oseltamivir acid, CAS 187227-45-8
规格 价格/CNY 货期 数量
1 mg ¥ 219 现货
5 mg ¥ 489 现货
10 mg ¥ 845 现货
25 mg ¥ 1,750 现货
50 mg ¥ 3,470 现货
100 mg ¥ 4,930 现货
500 mg ¥ 10,600 现货
1 mL * 10 mM (in DMSO) ¥ 485 现货
其他形式的 Oseltamivir acid:
产品目录号及名称: Oseltamivir acid (T5186)
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纯度: 98.88%
纯度: 98.29%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Oseltamivir acid (GS4071) is a potent influenza virus neuraminidase inhibitor and the prodrug of GS4071.
靶点活性 neuraminidase:100 nM.
体外活性 GS4071, a potent influenza virus neuraminidase inhibitor, was highly inhibitory to influenza A/NWS/33 (H1N1), A/Victoria/3/75 (H3N2), A/Shangdong/09/93 (H3N2) and B/Hong Kong/5/72 viruses in Madin Darby canine kidney (MDCK) cells. The 50% effective concentrations in these experiments ranged from 1.8 to 59.5 microM, with no cytotoxicity evident at 1000 microM [1]. Influenza B and A/H1N1 viruses were sensitive to oseltamivir (mean B IC50 value: 13 nM; mean H1N1 IC50 value: 1.34 nM). A/H1N2 and A/H3N2 viruses were more sensitive to oseltamivir (mean H3N2 IC50 value: 0.67 nM; mean H1N2 IC50 value: 0.9 nM) [2].
体内活性 The ethyl ester prodrug of GS4071, GS4104, administered by oral gavage (p.o.), had significant inhibitory effects on infections in mice induced by these viruses. No toxicity was seen in dosages up to 100 mg/kg/day. The minimum effective dosage for GS4104 was 0.1 mg/kg/day, with the compound administered twice daily for 5 days beginning 4 h pre-virus exposure. Oral therapy with GS4104 could be delayed from 48 to at least 60 h after exposure of mice to influenza A (H1N1) virus and still render a significant antiviral effect, the time of delay being dependent on the viral challenge dose [1]. Oseltamivir produced a dose-dependent antiviral effect against VN1203/04 in vivo. The 5-day regimen at 10 mg/kg/day protected 50% of mice; deaths in this treatment group were 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 [3].
动物实验 Female 6-week-old BALB/c mice were 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) was calculated after a 16-day observation period. Oseltamivir was 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 on the same schedule. Four hours after the first dose of oseltamivir, the mice were inoculated intranasally with 5 MLD50 of VN1203/04 virus in 50 μL of PBS. Survival and weight change were observed for 24 days. Virus titers in the mouse organs were determined on days 3, 6, and 9 after inoculation. Three mice from each experimental and placebo group were killed, and the lungs and brains were removed. The organs were homogenized and suspended in 1 mL of PBS. The cellular debris was cleared by centrifugation at 2000 g for 5 min. The limit of virus detection was 0.75 log10 EID50. For calculation of the mean, samples with a virus titer <0.75 log10 EID50/mL were assigned a value of 0. Virus titers in each organ were calculated by use of the method of Reed and Muench and are expressed as mean log10 EID50/mL ± SE [3].
别名 GS 4071, oseltamivir carboxylate, 奥斯他伟酸, Ro 64-0802
分子量 284.35
分子式 C14H24N2O4
CAS No. 187227-45-8

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 230 mg/mL (808.86 mM)

H2O: 56 mg/mL (196.94 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 3.5168 mL 17.584 mL 35.1679 mL 87.9198 mL
5 mM 0.7034 mL 3.5168 mL 7.0336 mL 17.584 mL
10 mM 0.3517 mL 1.7584 mL 3.5168 mL 8.792 mL
20 mM 0.1758 mL 0.8792 mL 1.7584 mL 4.396 mL
50 mM 0.0703 mL 0.3517 mL 0.7034 mL 1.7584 mL
100 mM 0.0352 mL 0.1758 mL 0.3517 mL 0.8792 mL

计算器

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稀释计算器
配液计算器
分子量计算器
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参考文献

1. Sidwell RW, et al. Inhibition of influenza virus infections in mice by GS4104, an orally effective influenza virus neuraminidase inhibitor. Antiviral Res. 1998 Feb;37(2):107-20. 2. Ferraris O, et al. Sensitivity of influenza viruses to zanamivir and oseltamivir: a study performed on viruses circulating in France prior to the introduction of neuraminidase inhibitors in clinical practice. Antiviral Res. 2005 Oct;68(1):43-8. 3. Yen HL, et al. Virulence may determine the necessary duration and dosage of oseltamivir treatment for highly pathogenic A/Vietnam/1203/04 influenza virus in mice. J Infect Dis. 2005 Aug 15;192(4):665-72.

文献引用

1. Luo D, Ye Q, Li R T, et al.PA-E18G substitution in influenza A virus confers resistance to ZX-7101, a cap-dependent endonuclease inhibitor.Virologica Sinica.2023
Anti-Influenza agent 5 BMY-27709 1-Deoxymannojirimycin hydrochloride Shegansu B Dihydromyricetin Tofacitinib Citrate Aurintricarboxylic acid Andrographolide

相关化合物库

该产品包含在如下化合物库中:
已知活性化合物库 上市药物库 抑制剂库 口服活性化合物库 经典已知活性库 抗COVID-19化合物库 表型筛选靶点鉴定库 血脑屏障通透化合物库 抗感染化合物库 FDA上市及药典收录分子库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
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给药体积
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动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Oseltamivir acid 187227-45-8 Metabolism Microbiology/Virology Drug Metabolite Influenza Virus GS-4071 Inhibitor GS 4071 oseltamivir carboxylate 奥斯他伟酸 Ro 64-0802 GS4071 inhibit inhibitor

 

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