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Linezolid
Cat# A5181
CAS# 165800-03-3
Background
Linezolid, a synthetic oxazolidinone antimicrobial, shows a wide spectrum against Gram-positive bacteria andmultidrug-resistant bacteria such as anaerobes, methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant enterococci, penicillin-resistant pneumococci and streptococcus [1,2].
Oxazolidinones could inhibit protein synthesis by binding to a site on the bacterial 23S ribosomal RNA of the 50S subunit and prevent the formation of a functional 70S-initiation complex. Linezolid is also a weak, nonselective and reversible inhibitor of monoamine oxidase [2].
In Vitro: Linezolid was a potent inhibitor of cell-free transcription-translation in E. coli. IC50 was 1.8 mM[3]. linezolid MICs vary slightly owing to the different test method and laboratory. The MIC values were between 0.5 and 4 mg/L for streptococci, enterococci and staphylococci [4].
Clinical Trials: Linezolid is fully bioavailable following oral administration, with maximum plasma linezolid concentrations achieved between 1 and 2 hours after oral administration. The elimination half-life of linezolid is 5–7 hours, and twice-daily administration of 400–600mg provides steady-state concentrations in the therapeutic range[5].
In clinical trials involving hospitalised patients with skin/soft tissue infections (predominantly S. aureus), intravenous/oral administration of linezolid (up to 1250 mg/day) produced clinical success in > 83% of individuals. In patients with community-acquired pneumonia, success rates were > 94%[6]. Linezolid could also be used in patients with nosocomial pneumonia[7].Linezolid appears to be well tolerated and the most common side effects is gastrointestinal disturbances [6].
Chemical Properties
| Physical Appearance |
A solid |
| Storage |
Store at -20°C |
| M.Wt |
337.35 |
| Cas No. |
165800-03-3 |
| Formula |
C16H20FN3O4 |
| Solubility |
≥16.85 mg/mL in DMSO; ≥2.48 mg/mL in H2O with gentle warming and ultrasonic; ≥9.5 mg/mL in EtOH with ultrasonic |
| Chemical Name |
N-[[(5S)-3-(3-fluoro-4-morpholin-4-ylphenyl)-2-oxo-1,3-oxazolidin-5-yl]methyl]acetamide |
| Canonical SMILES |
CC(=O)NCC1CN(C(=O)O1)C2=CC(=C(C=C2)N3CCOCC3)F |
| Shipping Condition |
Ship with blue ice, or upon other requests. |
| General tips |
For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon. |
Protocol
| Antibacterial test [1]: |
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Bacteria
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E. coli UC6782
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Preparation method
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The solubility of this compound in DMSO is > 16.9 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.
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Reacting condition
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0.01 ~ 1000 μM; 60 mins
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Applications
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Linezolid potently inhibited protein synthesis in E. coli UC6782, with the IC90 value of 30 μM. Linezolid was at least 2.5 times more potent than DuP-721 and about twice as potent as streptomycin.
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