Size | Price | Stock | Qty |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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ln Vitro |
Oseltamivir appears to be effective against influenza B and A/H1N1 viruses (mean B IC50 value: 13 nM; mean H1N1 IC50 value: 1.34 nM), but it is more effective against A/H1N2 and A/H3N2 viruses (average H3N2 IC50 value: 0.67 nM; average H1N2 IC50 value: 0.9 nM)[3]. The IC50 of RWJ-270201 (about 0.34 nM) in an influenza A virus neuraminidase inhibition experiment was similar to that of oseltamivir acid (0.45 nM). The B virus isolate RWJ-270201 has an IC50 of 1.36 nM, which is less than oseltamivir carboxylate (8.5 nM) and similar to zanamivir (2.7 nM) [4].
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ln Vivo |
The antiviral activity of oseltamivir acid (0.1, 1, or 10 mg/kg/day) on the Vietnam/1203/04 (VN1203/04) virus is dose-dependent. It is administered twice daily by borderline gavage. Fifty percent of the mice were protected by a 5-day treatment schedule of 10 mg/kg/day; the delayed death of the treated group suggests that the virus was still replicating after the treatment was stopped. Rationale: Doses of 1 and 10 mg/kg/day resulted in 60% and 80% morbidity, respectively, and significantly decreased viral titers in organs [5].
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References |
[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 |
Molecular Formula |
C14H24N2O4
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Molecular Weight |
284.356
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Exact Mass |
284.1736
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CAS # |
187227-45-8
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Related CAS # |
Oseltamivir;196618-13-0;Oseltamivir acid hydrochloride;1415963-60-8;Oseltamivir acid-d3;1242184-43-5;Oseltamivir phosphate;204255-11-8
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
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
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InChi Key |
(3R,4R,5S)-4-Acetamido-5-amino-3-pentan-3-yloxycyclohexene-1-carboxylic acid
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InChi Code |
NENPYTRHICXVCS-YNEHKIRRSA-N
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Chemical Name |
Oseltamivir carboxylate
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Synonyms |
GS-4071 Ro 64-0802 GS 4071 Ro-64-0802GS4071 Ro64-0802Oseltamivir acid
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HS Tariff Code |
2934.99.9001
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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 (e.g. under nitrogen), 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)
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Solubility (In Vitro) |
DMSO : ≥ 230 mg/mL (~808.86 mM)
H2O : ~125 mg/mL (~439.60 mM) |
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Solubility (In Vivo) |
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. 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. View More
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. 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. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.5167 mL | 17.5833 mL | 35.1667 mL | |
5 mM | 0.7033 mL | 3.5167 mL | 7.0333 mL | |
10 mM | 0.3517 mL | 1.7583 mL | 3.5167 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.