奥司他韦似乎对 B 型和 A/H1N1 流感病毒有效（平均 B IC50 值：13 nM；平均 H1N1 IC50 值：1.34 nM），但对 A/H1N2 和 A/H3N2 病毒更有效（平均 H3N2 IC50 值） ：0.67 nM；平均 H1N2 IC50 值：0.9 nM)[3]。 RWJ-270201在甲型流感病毒神经氨酸酶抑制实验中的IC50（约0.34 nM）与奥司他韦酸（0.45 nM）相似。 B 病毒分离株 RWJ-270201 的 IC50 为 1.36 nM，低于羧酸奥司他韦 (8.5 nM)，与扎那米韦 (2.7 nM) 相似[4]。

奥司他韦酸（0.1、1 或 10 mg/kg/天）对 Vietnam/1203/04 (VN1203/04) 病毒的抗病毒活性呈剂量依赖性。通过边缘管饲法每天两次施用。 50% 的小鼠受到 10 毫克/公斤/天的 5 天治疗方案的保护；治疗组的延迟死亡表明治疗停止后病毒仍在复制。理由：1 毫克/公斤/天和 10 毫克/公斤/天的剂量分别导致 60% 和 80% 的发病率，并显着降低器官中的病毒滴度 [5]。

[1]. Li W, et al. Identification of GS 4104 as an orally bioavailable prodrug of the influenza virus neuraminidase inhibitor GS 4071. Antimicrob Agents Chemother. 1998 Mar;42(3):647-53.
[2]. Ghosh GC, et al. Oseltamivir carboxylate, the active metabolite of oseltamivir phosphate (Tamiflu), detected in sewage discharge and river water in Japan. Environ Health Perspect. 2010 Jan;118(1):103-7.
[3]. 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.
[4]. Gubareva LV, et al. Comparison of the activities of zanamivir, oseltamivir, and RWJ-270201 against clinical isolates of influenza virus and neuraminidase inhibitor-resistant variants.Antimicrob Agents Chemother. 2001 Dec;45(12):3403-8.
[5]. 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.
[6]. Hoffmann G, et al. Nonclinical pharmacokinetics of oseltamivir and oseltamivir carboxylate in the central nervous system. Antimicrob Agents Chemother. 2009 Nov;53(11):4753-61

C14H24N2O4

284.356

284.1736

187227-45-8

Oseltamivir;196618-13-0;Oseltamivir acid hydrochloride;1415963-60-8;Oseltamivir acid-d3;1242184-43-5;Oseltamivir phosphate;204255-11-8

InChI=1S/C14H24N2O4/c1-4-10(5-2)20-12-7-9(14(18)19)6-11(15)13(12)16-8(3)17/h7,10-13H,4-6,15H2,1-3H3,(H,16,17)(H,18,19)/t11-,12+,13+/m0/s1

(3R,4R,5S)-4-Acetamido-5-amino-3-pentan-3-yloxycyclohexene-1-carboxylic acid

NENPYTRHICXVCS-YNEHKIRRSA-N

Oseltamivir carboxylate

GS-4071 Ro 64-0802 GS 4071 Ro-64-0802GS4071 Ro64-0802Oseltamivir acid

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ≥ 230 mg/mL (~808.86 mM)
H2O : ~125 mg/mL (~439.60 mM)

Solubility in Formulation 1: ≥ 5.75 mg/mL (20.22 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 57.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 5.75 mg/mL (20.22 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 57.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 5.75 mg/mL (20.22 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 57.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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Solubility in Formulation 4: 100 mg/mL (351.68 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。