Size | Price | Stock | Qty |
---|---|---|---|
250mg |
|
||
500mg |
|
||
1g |
|
||
2g |
|
||
5g |
|
||
10g |
|
||
Other Sizes |
|
Purity: ≥98%
Oseltamivir phosphate (GS 4104;Tamiflu) is a potent neuraminidase inhibitor and an approved antiviral drug that has been widely used for the treatment and prophylaxis of influenza A and B. Oseltamivir is taken orally. The Infectious Disease Society of America, the United States' Centers for Disease Control and Prevention (CDC), and the United Kingdom's National Institute for Health and Care Excellence recommend the use of oseltamavir for people who have complications or are at high risk for complications who present within 48 hours of first symptoms of infection. They recommend its use to prevent infection in at-risk people but not the general population. The CDC recommends that clinicians use their discretion to treat those at lower risk who present within 48 hours of first symptoms of infection.
ln Vitro |
After oral treatment, oseltamivir phosphate (OP) is a prodrug that is easily absorbed from the gastrointestinal tract. Hepatic esterases are primarily responsible for the prodrug's substantial conversion to oseltamivir carboxylate (OC) [1]. One commonly used anti-influenza sialidase inhibitor is oseltamivir phosphate. The metabolic activity of CMA07 and CMT-U27 cell lines was considerably decreased following 305 μM oseltamivir phosphate treatment (p=0.005 and p<0.0001, respectively), according to a one-way ANOVA test. On the other hand, when oseltamivir phosphate was treated at 0.305 μM (p=0.9781), 3.05 μM (p=0.7436), and 30.5 μM (p=0.9623) in contrast to control cells, no statistically significant changes were seen. In order to assess the impact of oseltamivir phosphate on CMA07 and CMT-U27 programmed cell death, the TUNEL test was employed, taking into account that 305 μM oseltamivir phosphate administration reduces cellular metabolic activity. When compared to lower oseltamivir concentrations or PBS, 24-hour oseltamivir phosphate administration, specifically 305 μM, significantly increased CMA07 (p=0.001) and CMT-U27 (p=0.0002) DNA fragmentation[2].
|
---|---|
ln Vivo |
Ki-67 antigen and caspase-3 protein were used to assess CMT-U27 xenograft tumor cell proliferation and apoptosis, respectively. Almost no differences were found in Ki-67 and caspase 3 (p=0.2) expression between oseltamivir-treated and untreated mice [2]. Oseltamivir phosphate-treated mice showed significantly more inflammatory infiltrates in primary tumors (p=0.01).
|
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 |
Molecular Formula |
C16H31N2O8P
|
---|---|
Molecular Weight |
410.3997
|
CAS # |
204255-11-8
|
Related CAS # |
Oseltamivir;196618-13-0;Oseltamivir acid;187227-45-8;Oseltamivir-d5 phosphate;Oseltamivir-d3 phosphate
|
Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
SMILES |
O=C(C1=C[C@@H](OC(CC)CC)[C@H](NC(C)=O)[C@@H](N)C1)OCC.O=P(O)(O)O
|
InChi Key |
PGZUMBJQJWIWGJ-ONAKXNSWSA-N
|
InChi Code |
InChI=1S/C16H28N2O4.H3O4P/c1-5-12(6-2)22-14-9-11(16(20)21-7-3)8-13(17)15(14)18-10(4)19;1-5(2,3)4/h9,12-15H,5-8,17H2,1-4H3,(H,18,19);(H3,1,2,3,4)/t13-,14+,15+;/m0./s1
|
Chemical Name |
ethyl (3R,4R,5S)-4-acetamido-5-amino-3-pentan-3-yloxycyclohexene-1-carboxylate;phosphoric acid
|
Synonyms |
GS-4071, GS-4104, GS4071, GS4104, GS 4071, GS 4104, Tamiflu
|
HS Tariff Code |
2934.99.9001
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
H2O : ~100 mg/mL (~243.66 mM)
DMSO : ~100 mg/mL (~243.66 mM) |
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.09 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 25.0 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.09 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 25.0 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.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.