Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 230 mg/mL (808.86 mM)
H2O: 56 mg/mL (196.94 mM)
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 |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
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