Oseltamivir phosphate (Synonyms: GS4104, Ro 640796/002) |
| Catalog No.GC15396 |
Oseltamivir phosphate(GS 4104)는 인플루엔자 A 및 B의 치료 및 예방에 권장되는 뉴라미니다제 억제제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 204255-11-8
Sample solution is provided at 25 µL, 10mM.
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Oseltamivir phosphate (GS 4104) is a neuraminidase inhibitor recommended for the treatment and prophylaxis of influenza A and B.
Oseltamivir phosphate (OP) is a prodrug that is readily absorbed from the gastrointestinal tract after oral administration and is extensively converted predominantly by hepatic esterases to Oseltamivir carboxylate (OC)[1]. Oseltamivir phosphate is a widely used anti-influenza sialidase inhibitor. The metabolic activity of CMA07 and CMT-U27 cell lines is significantly decreased with 305 μM Oseltamivir phosphate treatment (p=0.005 and p<0.0001 respectively) using One Way ANOVA testes. In contrast, no statistically significant alterations are observed with 0.305 μM (p=0.9781), 3.05 μM (p=0.7436) and 30.5 μM (p=0.9623) of Oseltamivir phosphate treatments when compare with control cells. Finally, to assess the effect of Oseltamivir phosphate on CMA07 and CMT-U27 programmed cell death, and given that 305 μM Oseltamivir phosphate treatment impaired cell metabolic activity, a programmed cell death measurement is performed with the TUNEL assay. Twenty-four hour Oseltamivir phosphate treatment, specifically at 305 μM, significantly increases CMA07 (p=0.001) and CMT-U27 (p=0.0002) DNA fragmentation, suggesting promotion of programmed cell death, when compare with lower Oseltamivir concentrations, or with PBS[2].
Oseltamivir phosphate-treated mice present significantly more inflammatory infiltrate in primary tumors (p=0.01). Ki-67 antigen and caspase-3 protein are used to assess CMT-U27 xenograft tumor cell proliferation and apoptosis respectively. Virtually no differences are found in Ki-67 and caspase 3 (p=0.2) expression between Oseltamivir-treated and non-treated mice[2].
References:
[1]. Huang H, et al. Transplacental transfer of Oseltamivir phosphate and its metabolite Oseltamivir carboxylate using the ex vivo human placenta perfusion model in Chinese Hans population. J Matern Fetal Neonatal Med. 2016 Aug 8:1-5.
[2]. de Oliveira JT, et al. Anti-influenza neuraminidase inhibitor Oseltamivir phosphate induces canine mammary cancer cell aggressiveness. PLoS One. 2015 Apr 7;10(4):e0121590.
[3]. Li P, et al. A Simple and Robust Approach for Evaluation of Antivirals Using a Recombinant Influenza Virus Expressing Gaussia Luciferase. Viruses. 2018 Jun 13;10(6). pii: E325.
| Cell experiment [1]: | |
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Cell lines |
MDCK cells |
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Preparation method |
The solubility of this compound in DMSO is limited. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
|
Reacting condition |
0 ~ 12 μM |
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Applications |
Oseltamivir Phosphate exhibited inhibitory effects against both H5N1 and H9N2 viruses. In MDCK cells, the active metabolite of Oseltamivir Phosphate reduced viral replication with the EC50 values ranging from 7.5 to 12 μM, and reduced neuraminidase activity with the IC50 values ranging from 7.0 to 15 nM. |
| Animal experiment [1]: | |
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Animal models |
Mice infected with A/HK/156/97 (H5N1) or A/Qa/HK/G1/97 (P3) |
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Dosage form |
0.1, 1, 10 and 100 mg/kg/d; p.o. |
|
Applications |
In mice infected with H5N1, Oseltamivir Phosphate significantly decreased the titer of virus in the lungs. However, the reduction in virus titer was almost the same as between the 1 and 10 mg/kg/d dose groups and the 100 mg/kg/d dose group. In mice infected with P3, Oseltamivir Phosphate at the doses of 1 and 10 mg/kg/d also significantly reduced the virus titer in lungs, and a dose of 100 mg/kg/d Oseltamivir Phosphate completely inhibited virus replication. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Leneva IA, Roberts N, Govorkova EA, Goloubeva OG, Webster RG. The neuraminidase inhibitor GS4104 (oseltamivir phosphate) is efficacious against A/Hong Kong/156/97 (H5N1) and A/Hong Kong/1074/99 (H9N2) influenza viruses. Antiviral Res. 2000 Nov;48(2):101-15. |
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| Cas No. | 204255-11-8 | SDF | |
| Synonyms | GS4104, Ro 640796/002 | ||
| Chemical Name | 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 | ||
| Formula | C16H31N2O8P | M.Wt | 410.4 |
| Solubility | 100 mg/mL in DMSO ( Need ultrasonic); 100 mg/mL in Water ( Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4366 mL | 12.1832 mL | 24.3665 mL |
| 5 mM | 0.4873 mL | 2.4366 mL | 4.8733 mL |
| 10 mM | 0.2437 mL | 1.2183 mL | 2.4366 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 40 reference(s) in Google Scholar.)
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