1. Anti-infection
    Metabolic Enzyme/Protease
  2. Influenza Virus
    Drug Metabolite

Oseltamivir acid (Synonyms: GS 4071; Ro 64-0802; oseltamivir carboxylate)

Cat. No.: HY-13318 Purity: 98.60%
Handling Instructions

GS 4104, the ethyl ester prodrug of GS 4071, is an inhibitor of influenza virus neuraminidase with an IC50 of approximately 100 nM.

For research use only. We do not sell to patients.

Oseltamivir acid Chemical Structure

Oseltamivir acid Chemical Structure

CAS No. : 187227-45-8

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Other Forms of Oseltamivir acid:

Top Publications Citing Use of Products

    Oseltamivir acid purchased from MCE. Usage Cited in: Antiviral Res. 2016 May;129:81-92.

    MDCK cells are infected with K435E or H274Y in the absence of compounds and maintained at 35 °C in agarose with or without 10 nM Oseltamivir or 20 μg/mL D35, respectively.

    Oseltamivir acid purchased from MCE. Usage Cited in: Antiviral Res. 2014 Nov;111:69-77.

    Plaque formation of different recombinant viruses in the presence of oseltamivir. MDCK cells are infected with recombinant viruses in the absence of Oseltamivir or DS and maintained in agarose overlay medium with 50 nM Oseltamivir or 100 μg/mL DS (DS), or without compounds (None) at 35 °C.

    Oseltamivir acid purchased from MCE. Usage Cited in: PLoS One. 2016 May 27;11(5):e0156400.

    Live-cell fluorescence imaging of infected cells of Oseltamivir-resistant virus. MDCK cells are infected with Oseltamivir-resistant 738 and -sensitive 838. After incubation at 37°C for 12 hr, the cells are incubated with BTP3-Neu5Ac with or without Oseltamivir or Zanamivir (each 100 nM for final concentrations) in an SFM at 37°C for 10 min. Fluorescent images of the cells are observed under UV irradiation by using a fluorescence microscope. A scale bar indicates 200 μm.

    Oseltamivir acid purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Jan;97:385-394.

    The inhibitory effects of OA on M1 protein synthesis and in three different infection protocols. M1 protein expression in H1N1-infected MDCK cells analyzed by Western blot 24 h post infection.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    GS 4104, the ethyl ester prodrug of GS 4071, is an inhibitor of influenza virus neuraminidase with an IC50 of approximately 100 nM.

    IC50 & Target

    Influenza A and B[1]

    In Vitro

    Oseltamivir acid inhibits virus replication in vitro and in vivo. Influenza B and A/H1N1 viruses appeare to be sensitive to Oseltamivir (mean B IC50 value: 13 nM; mean H1N1 IC50 value: 1.34 nM), while A/H1N2 and A/H3N2 viruses are more sensitive to Oseltamivir (mean H3N2 IC50 value: 0.67 nM; mean H1N2 IC50 value: 0.9 nM)[1]. In neuraminidases inhibition assays with influenza A viruses, the median 50% inhibitory concentration (IC50) of RWJ-270201 (approximately 0.34 nM) is comparable to that of Oseltamivir carboxylate (0.45 nM) For influenza B virus isolates, the IC50 of RWJ-270201 (1.36 nM) is comparable to that of Zanamivir (2.7 nM) and less than that of Oseltamivir carboxylate (8.5 nM)[2].

    In Vivo

    Oseltamivir (0.1, 1, or 10 mg/kg/day, twice daily by oral gavage) produces a dose-dependent antiviral effect against Vietnam/1203/04 (VN1203/04) virus. The 5-day regimen at 10 mg/kg/day protects 50% of mice; deaths in this treatment group are delayed and indicated the replication of residual virus after the completion of treatment. Eight-day regimens improved Oseltamivir efficacy, and dosages of 1 and 10 mg/kg/day significantly reduced virus titers in organs and provided 60% and 80% survival rates, respectively[3]. In the pharmacokinetic study, after the oral administration of 1,000 mg/kg Oseltamivir, peak plasma concentrations are reached at 2 h postdose for Oseltamivir and 8 h for Oseltamivir carboxylate (OC). Rats are exposed to Oseltamivir over the whole sampling interval and had a ~2.7-fold-higher rate of exposure to OC than Oseltamivir. In CSF, peak concentrations are reached at 2 h postdose for Oseltamivir and 6 h for OC. CSF/plasma exposure ratios (AUC0-8 h) are ~0.07 for Oseltamivir and 0.007 for OC. In perfused brain samples, peak concentrations are reached at 8 h postdose for Oseltamivir and 6 h for OC. Brain/plasma exposure ratios (AUC0-8 h) of ~0.12 for Oseltamivir and 0.01 for OC are recorded. Corresponding CSF/brain exposure ratios ranged between ~0.55 and 0.64 for both analytes. A further group of animals that received a single oral administration of Oseltamivir at a lower dose produced similar results[4].

    Solvent & Solubility
    In Vitro: 

    H2O : ≥ 56 mg/mL (196.94 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.5168 mL 17.5840 mL 35.1679 mL
    5 mM 0.7034 mL 3.5168 mL 7.0336 mL
    10 mM 0.3517 mL 1.7584 mL 3.5168 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Animal Administration
    [3][4]

    Mice[3]
    Female 6-week-old BALB/c mice are anesthetized with isofluorane and intranasally inoculated with 50 μL of 10-fold serial dilutions of VN1203/04 virus in PBS. The mouse lethal dose (MLD50) is calculated after a 16-day observation period. Oseltamivir is administered by oral gavage twice daily for 5 or 8 days to groups of 10 mice at dosages of 0.1, 1, and 10 mg/kg/day. Control (infected but untreated) mice received sterile PBS (placebo) on the same schedule. Four hours after the first dose of Oseltamivir, the mice are inoculated intranasally with 5 MLD50 of VN1203/04 virus in 50 μL of PBS. Survival and weight change are observed for 24 days. Virus titers in the mouse organs are determined on days 3, 6, and 9 after inoculation. Three mice from each experimental and placebo group are killed, and the lungs and brains are removed. The organs are homogenized and suspended in 1 mL of PBS. The cellular debris is cleared by centrifugation at 2000 g for 5 min. The limit of virus detection is 0.75 log10 EID50. For calculation of the mean, samples with a virus titer <0.75 log10 EID50/mL are assigned a value of 0. Virus titers in each organ are calculated by use of the method of Reed and Muench and are expressed as mean log10 EID50/mL±SE.
    Rats[4]
    Several studies are performed to characterize the pharmacokinetics of Oseltamivir and OC in the plasma, cerebrospinal fluid (CSF), and brain of Sprague-Dawley rats following single-dose bolus administration of Oseltamivir (intravenous [i.v.] and oral) and OC (i.v.). In the i.v. studies, nonfasted adult rats (two groups of 35 animals for each test substance) received a dose of 30 mg/kg body weight of either Oseltamivir or Oseltamivir carboxylate (OC) in aqueous solution with sodium chloride (0.9%; pH 4.0) via slow injection into the tail vein over 20 to 30 s. In both i.v. studies, pharmacokinetic sampling took place at 5 min and at 0.25, 0.5, 1, 2, 4, and 8 h postdose (four or five rats/time point).

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    284.35

    Formula

    C₁₄H₂₄N₂O₄

    CAS No.

    187227-45-8

    SMILES

    O=C(O)C1=C[[email protected]]([[email protected]@H]([[email protected]](C1)N)NC(C)=O)OC(CC)CC

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

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    Product Name:
    Oseltamivir acid
    Cat. No.:
    HY-13318
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    Oseltamivir acid

    Cat. No.: HY-13318