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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。
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 | 库存 | 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 x 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 | Oseltamivir acid 是一种高效的流感病毒神经氨酸酶抑制剂,在Madin Darby犬肾 (MDCK) 细胞中对A/NWS/33 (H1N1)、A/Victoria/3/75 (H3N2)、A/Shangdong/09/93 (H3N2) 和B/Hong Kong/5/72 病毒有强烈的抑制作用。这些实验中50%有效浓度范围为1.8至59.5 microM,且在1000 microM浓度下未见明显的细胞毒性 [1]。流感B型和A/H1N1病毒对奥司他韦敏感(平均B型IC50值:13 nM;平均H1N1 IC50值:1.34 nM)。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)[2]。 |
体内活性 | GS4104,Oseltamivir acid的乙酯前药,通过口腔灌胃(p.o.)给药,在由这些病毒引起的小鼠感染中显示出显著的抑制效果。在高达100 mg/kg/天的剂量下未见毒性。GS4104的最小有效剂量为0.1 mg/kg/天,此化合物需每日两次给药,连续5天,从暴露病毒前4小时开始给药。即使在小鼠暴露于流感A (H1N1)病毒后48至至少60小时开始口服GS4104治疗,仍能显著产生抗病毒效果,延迟时间取决于病毒挑战剂量 [1]。Oseltamivir对VN1203/04的体内抗病毒效果呈剂量依赖性。5天给药方案,以每天10 mg/kg的剂量保护了50%的小鼠;此治疗组中的死亡延迟,表明治疗完成后残留病毒的复制。8天给药方案提高了oseltamivir的效果,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%的生存率 [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, Ro 64-0802, 奥斯他伟酸 |
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 | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 16.67 mg/mL (58.61 mM), Sonication is recommended. H2O: 56 mg/mL (196.94 mM) | ||||||||||||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||||||||||||
DMSO/H2O
H2O
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