SKU: L007  / 
    CAS Number: 165800-03-3

    Linezolid

    RM712.50 - RM1,303.88
    Linezolid

    Linezolid is an oxazolidinone antibiotic and is effective against Gram-positive bacteria including certain strains of methicillin-resistant Staphylococcus aureus (MRSA).  Linezolid was discovered in the mid-1990s and was approved for commercial use in 2000.  The crystal structure was elucidated in 2008 by Yale researchers. The compound is synthetic, and many apporaches for Linezolid synthesis have been reported.  It is active against Gram-positive bacteria including certain methicillin-resistant Staphylococcus aureus (MRSA).

    Mechanism of Action Linezolid inhibits protein synthesis by binding to the 50S ribosomal subunit (23S rRNA) which prevents formation of the 70S initiation complex thus inhibiting mRNA translation. The initiation complex is composed of the 30S, 50S ribosome subunits, tRNAa nd mRNA.  Since this mechanism is unique, cross-resistance between linezolid and other protein synthesis inhibitors is highly infrequent or nonexistent.  It is also a nonselective monoamine oxidase (MAO) inhibitor displaying nonselective, reversible binding.
    Spectrum Linezolid is active against Gram-positive bacteria including certain strains of methicillin-resistant Staphylococcus aureus (MRSA).  It is bacteriocidal against the majority of streptococcal strains and bacteriostatic against staphylococci and enterococci.  It is also active in vitro against several mycobacteria.  In vitro, it is active on select Gram-negative bacteria but does not have any activity in vivo on clinically significant species.
    Eukaryotic Cell Culture Applications Linezolid inhibits cytokine production from human peripheral blood monocytes in a dose-dependent manner. Linezolid was found to modify the acute phase inflammatory response. Linezolid inhibits cytokine production from human peripheral blood monocytes in a dose-dependent manner (Garcia-Roca et al, 2006).
    Molecular Formula C16H20FN3O4
    References

    Ament PW (2002)   Linezolid: Its role in the treatment of Gram-positive, drug-resistant bacterial infections. Amer. Family Phys. 65(4):663-671  PMID  11871684 

    Champney WS and Miller M (2002)  Linezolid is a specific inhibitor of 50S ribosomal subunit formation in Saphylococcus aureus cells. Curr. Microbiol. 44(5):350-356  PMID 11927986

    Garcia-Roca P, Mancilla-Ramirez J, Santos-Segura A, Fernandez-Aviles M, Calderon-Jaimes E (2006)  Linezolid diminishes inflammatory cytokine production from human peripheral blood mononuclear cells. 37(1):31-35  PMID 16314183

    Herrmann DJ et al (2008)  Linezolid for the treatment of drug-resistant infections. Expert Rev. Anti Infect. Ther. 6(6):825-648  PMID 19053895

    Shinabarger DL (1997)  Mechanism of action of Oxazolidinones: Effects of Linezolid and Eperezolid on translation reactions.  Antimicrob. Agents Chemother. 41(10):2132-2136  PMID 9333037