Oseltamivir phosphate是一种流感神经氨酸酶抑制剂，对Influenza B，A/H1N1，A/H1N2和A/H3N2 病毒的IC₅₀值分别为13nM，1.34nM，0.9nM和0.67nM。
Cas No.:204255-11-8
Sample solution is provided at 25 µL, 10mM.
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Oseltamivir phosphate is an inhibitor of influenza neuraminidase, with IC₅₀ values of 13nM, 1.34nM, 0.9nM, and 0.67nM against Influenza B, A/H1N1, A/H1N2, and A/H3N2 viruses, respectively[1]. As a neuraminidase inhibitor, Oseltamivir phosphate attenuates the penetration of viruses through the mucus on the respiratory tract and inhibits the release of virus progeny from infected cells[2].
In vitro, with 3 days of treatment, Oseltamivir phosphate at 0.0125nM showed partial inhibition, whereas concentrations above 0.05nM showed complete inhibition in H1N1 IVA-infected MDCK cells[2]. Oseltamivir phosphate (500-800μg/mL; 24-72h) inhibited the viability of MDA-MB-231 and MCF-7 cells in a dose- and time-dependent manner[3].
In vivo, in BALB/c mice infected with the H3N1 influenza virus, Oseltamivir phosphate (1 and 10mg/kg/d; p.o.; twice daily from 4 hours before infection to 5 days post-infection) dose-dependently reduced total cells, neutrophils, macrophages, and pro-inflammatory cytokines in bronchoalveolar lavage fluid (BALF)[4].
References:
[1] Ferraris, O et al. “Sensitivity of influenza viruses to zanamivir and Oseltamivir phosphate: a study performed on viruses circulating in France prior to the introduction of neuraminidase inhibitors in clinical practice.” Antiviral research vol. 68,1 (2005): 43-8.
[2] Chan RWY, Tao KP, Ye J, et al. Inhibition of Influenza Virus Replication by Oseltamivir phosphate Derivatives. Pathogens. 2022;11(2):237.
[3] Haxho F, Allison S, Alghamdi F, et al. Oseltamivir phosphate phosphate monotherapy ablates tumor neovascularization, growth, and metastasis in mouse model of human triple-negative breast adenocarcinoma. Breast Cancer (Dove Med Press). 2014;6:191-203.
[4] Wong ZX, Jones JE, Anderson GP, Gualano RC. Oseltamivir phosphate treatment of mice before or after mild influenza infection reduced cellular and cytokine inflammation in the lung. Influenza Other Respir Viruses. 2011;5(5):343-350.
Oseltamivir phosphate是一种流感神经氨酸酶抑制剂，对Influenza B，A/H1N1，A/H1N2和A/H3N2 病毒的IC₅₀值分别为13nM，1.34nM，0.9nM和0.67nM[1]。作为一种神经氨酸酶抑制剂，Oseltamivir phosphate可以减弱病毒通过呼吸道粘液的渗透，并抑制病毒子代从感染细胞释放[2]。
体外实验中，经3天处理，Oseltamivir phosphate在0.0125nM时对H1N1 IVA感染的MDCK细胞表现为部分抑制，而在高于0.05nM的浓度下表现为完全抑制[2]。Oseltamivir phosphate（500-800μg/mL；24-72h）以剂量依赖和时间依赖的方式抑制MDA-MB-231和MCF-7细胞的活力[3]。
体内实验中，在感染H3N1流感病毒的BALB/c小鼠中，Oseltamivir phosphate（1和10mg/kg/天；灌胃；自感染前4小时至感染后5天，每日2次）以剂量依赖方式降低支气管肺泡灌洗液（BALF）中的总细胞数、中性粒细胞、巨噬细胞及促炎性细胞因子水平[4]。
| Cell experiment [1]: | |
Cell lines | MDCK cells infected with the H1N1 IVA virus |
Preparation Method | The inhibitory dose range of Oseltamivir phosphate was tested by adding 100 TCID50 of IVA447 to the MDCK cells. Cells were first washed with PBS, and replenished with 100ul medium containing Oseltamivir phosphate of respective concentrations for 72h. |
Reaction Conditions | 0-12.8nM; 72h |
Applications | Partial rescue of the cells was observed with Oseltamivir phosphate treatment at 0.0125nM and exerted complete inhibition at more than 0.05nM. |
| Animal experiment [2]: | |
Animal models | RAGxCγ double mutant mice bearing heterotopic xenografts of MDA-MB-231 tumors |
Preparation Method | Treatment with 30mg/kg and 50mg/kg of soluble Oseltamivir phosphate in sterile saline were injected daily intraperitoneally starting at day 10 postimplantation, when the tumor volumes reached 10-20mm3. For the 50mg/kg Oseltamivir phosphate cohort, the daily treatment regimen continued to day 111, then once a week until day 124, when the mice were taken off the drug treatment. |
Dosage form | 30mg/kg and 50mg/kg; i.p. |
Applications | Treatment with 30mg/kg and 50mg/kg of soluble Oseltamivir phosphate in sterile saline with daily injections intraperitoneally at day 10 postimplantation when the tumor volume reached 10-20mm3 attenuated the aggressive tumor vascularization with skin lesions and the tumor growth. Live tumor weight per mouse body weight indicated a significant reduction for the Oseltamivir phosphate 30mg/kg cohort at days 32-42 compared to the untreated cohort. There were no visible tumors for the 50mg/kg Oseltamivir phosphate cohort at day 180. The survival rate of the 50mg/kg Oseltamivir phosphate-treated cohort was significant compared to the untreated control group. The daily dosage of 30mg/kg and 50mg/kg Oseltamivir phosphate treatment intraperitoneally, significantly attenuated the metastatic spread of MDA-MB-231 breast cancer cells to the lungs compared to the extensive metastatic clusters of cancer cells in the lungs for the untreated cohort. |
References: | |
| Cas No. | 204255-11-8 | SDF | |
| 别名 | 磷酸奥司他韦; GS 4104 | ||
| 化学名 | ethyl (3R,4R,5S)-4-acetamido-5-amino-3-pentan-3-yloxycyclohexene-1-carboxylate;phosphoric acid | ||
| Canonical SMILES | CCC(CC)OC1C=C(CC(C1NC(=O)C)N)C(=O)OCC.OP(=O)(O)O | ||
| 分子式 | C16H31N2O8P | 分子量 | 410.4 |
| 溶解度 | 100 mg/mL in DMSO ( Need ultrasonic); 100 mg/mL in Water ( Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4366 mL | 12.1832 mL | 24.3665 mL |
| 5 mM | 487.3 μL | 2.4366 mL | 4.8733 mL |
| 10 mM | 243.7 μL | 1.2183 mL | 2.4366 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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