SKU: O041

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Description
Oseltamivir Phosphate is an inhibitor of influenza viral neuraminidase.  It is also an antiviral used against influenza A and B.  Oseltamivir was discovered at Gilead.

    CAS Number

    204255-11-8

    Molecular Formula

    C16H28N2O4 ∙ H3PO4

    Molecular Weight

    410.40

    Mechanism of Action

    Oseltamivir Phosphate is converted to its active form (Oseltamivir Carboxylate) in vivo by hepatic esterases via ester hydrolysis. Oseltamivir Carboxylate inhibits influenza viral neuraminidase, an enzyme which cleaves sialic acid residues. The result is that the newly replicated virus cannot be released from infected cells of the respiratory tract and thus cannot replicate.

    Storage Conditions

    -20°C

    Tariff Code

    2924.29.9500

    Spectrum

    Oseltamivir is broad-spectrum against a range of influenza A and B subtypes, due to the conserved nature of the neuraminidase enzyme, which is highly selective for influenza only (neuraminidase A and B). It is effective for human seasonal viruses, avian viruses, and pandemic viruses including H1N1 virus.

Applications

    Cancer Applications

    THe antitumor activity of Oseltamivir Phosphate was studied in a mouse model with human triple-negative breast adenocarcinoma using MCF-7 and MDA-MB-231 cell lines. The compound was able to completely ablate tumor vascularization, tumor growth, and spread to the lungs when used at 50 mg/kg (Haxho et al, 2014).

    Microbiology Applications

    Oseltamivir Phosphate IC50 range for influenza A and B subtypes is ≤ 1 nM - 30 nM. Resistance to Oseltamivir is due to single amino acid residue substitutions (His274Tyr in N1) in the neuraminidase enzyme.

Specifications

    Form

    Powder

    Appearance

    White to off-white powder

    Source

    Synthetic

References

    References

    Davies BE (2010) Pharmacokinetics of Oseltamivir: An oral antiviral for the treatment and prophylaxis of influenza in diverse populations. J. Antimicrob. Chemother. 65(S2):ii5-iii10 PMID 20215135 Govorkova EA et al (2009) Susceptibility of highly pathogenic H5N1 influenza viruses to the neuraminidasei ihibitor Oseltamivir differs in vitro and in a mouse model. Antimicrob. Agents Chemother. 53 (7) 3088-3096 Haxho F et al (2014) Oseltamivir phosphate monotherapy ablates tumor neovascularization, growth, and metastatis in mouse model of human triple-negative breast adenocarcinoma. Breast Cancer 6:191-203 PMID 25525387 Kamal MA(2015) A drug-disease model describing the effect of Oseltamivir neuraminidase inhibition on influenza virus progression. Antimicrob Agents Chemother. 59(9):5388-5395. PMID 26100715

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