For research use only.
Licensed by Pfizer Catalog No.S1408
CAS No. 165800-03-3
Linezolid (PNU-100766) is a synthetic antibiotic used for the treatment of serious infections.
Selleck's Linezolid (PNU-100766) has been cited by 15 publications
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Auranofin inhibits MRSA toxin production and effectively clears intracellular bacteria. (a) Toxin production (ng/ml) in S. aureus MRSA USA300 after treatment with auranofin or control antibiotics (linezolid or vancomycin) for one hour (data corrected for organism burden). The results are presented as mean ± SD (n = 3). Statistical analysis was done by two-tailed Student’s ‘t’ test. Asterisks (**) indicate statistical significance in relation to the control (DMSO or water). P values of (**P ≤ 0.01) are considered significant. Detailed “P” values are listed below. α-hemolysin: control vs linezolid: 0.0027, control vs auranofin: 0.001. Panton-Valentine leukocidin: control vs linezolid: 0.0017, control vs auranofin: 0.0040. (b) MRSA USA300 infected J774A.1 cells were treated with auranofin and control antibiotics (vancomycin or linezolid) for 24 hours and the percent bacterial reduction was calculated compared to untreated control groups. The results are given as mean ± SD (n = 3). Two-tailed Student’s ‘t’ test was employed and P values of (*,# ≤ 0.05) are deemed significant. Auranofin was compared to controls (*) and to antibiotics (#). Detailed “P” values are listed below. Control vs linezolid: 0.0234, control vs vancomycin: 0.021, control vs auranofin: 0.02031, linezolid vs auranofin: 0.0397, vancomycin vs auranofin: 0.0491.
Sci Rep, 2016, 6:22571. Linezolid (PNU-100766) purchased from Selleck.
Efficacy of treatment of meticillin-resistant Staphylococcus aureus (MRSA) murine skin lesions with auranofin 0.5%, 1% and 2%, linezolid and clindamycin (25 mg/kg), mupirocin (2%), fusidic acid (2%) and petroleum jelly (control). Statistical analysis was performed by the two-tailed Student's t-test. *,# P-values of ≤0.05 were considered significant; auranofin was compared both with controls (*) and with antibiotics (#).
Int J Antimicrob Agents, 2016, 47(3):195-201. Linezolid (PNU-100766) purchased from Selleck.
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|Description||Linezolid (PNU-100766) is a synthetic antibiotic used for the treatment of serious infections.|
Linezolid inhibits initiation complex formation with either the 30S or the 70S ribosomal subunits from Escherichia coli. Linezolid inhibits complex formation with Staphylococcus aureus 70S tight-couple ribosomes.  Linezolid is a potent inhibitor of cell-free transcription-translation in E. coli, exhibiting 50% inhibitory concentrations (IC50s) of 1.8 mM.  Linezolid is an oxazolidinone, a new class of antibacterial agents with enhanced activity against pathogens.  Linezolid MICs vary slightly with the test method, laboratory, and significance attributed to thin hazes of bacterial survival, but all workers find that the susceptibility distributions are narrow and unimodal, with MIC values between 0.5 and 4 mg/L for streptococci, enterococci and staphylococci. Linezolid entails mutation of the 23S rRNA that forms the binding site.  Linezolid is an oxazolidinone whose mechanism of action involves inhibition of protein synthesis at a very early stage. Linezolid is added to 7H10 agar medium (Difco) supplemented with OADC (oleic acid, albumin, dextrose, and catalase) at 50°C to 56°C by doubling the dilutions to yield a final concentration of 0.125 μg/mL to 4 μg/mL. Linezolid shows excellent in vitro activity against all the strains tested (MICs ≤ 1 μg/ml), including those resistant to SIRE. 
-  Swaney SM, et al. Antimicrob Agents Chemother, 1998, 42(12), 3251-3255.
-  Shinabarger DL, et al. Antimicrob Agents Chemother, 1997, 41(10), 2132-2136.
-  Noskin GA, et al. Antimicrob Agents Chemother, 1999, 43(8), 2059-2062.
|In vitro||DMSO||67 mg/mL (198.6 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
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Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03537495||Recruiting||Drug: Linezolid||Tuberculosis Meningeal|Linezolid||Universitas Padjadjaran|Radboud University|Global Alliance for TB Drug Development||April 21 2021||Phase 2|
|NCT04239326||Recruiting||Diagnostic Test: targeted Next Generation Sequencing (tNGS)||Tuberculosis Multidrug-Resistant||Foundation for Innovative New Diagnostics Switzerland||April 16 2021||--|
|NCT04775238||Recruiting||Other: Silver nanoparticles|Other: Copper nanoparticles||Nosocomial Infections||Sohag University||February 27 2021||Not Applicable|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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