Linezolid (PNU-100766)

Licensed by Pfizer Catalog No.S1408

For research use only.

Linezolid (PNU-100766) is a synthetic antibiotic used for the treatment of serious infections.

Linezolid (PNU-100766) Chemical Structure

CAS No. 165800-03-3

Selleck's Linezolid (PNU-100766) has been cited by 15 publications

Purity & Quality Control

Choose Selective Antibiotics Inhibitors

Biological Activity

Description Linezolid (PNU-100766) is a synthetic antibiotic used for the treatment of serious infections.
In vitro

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. [1] Linezolid is a potent inhibitor of cell-free transcription-translation in E. coli, exhibiting 50% inhibitory concentrations (IC50s) of 1.8 mM. [2] Linezolid is an oxazolidinone, a new class of antibacterial agents with enhanced activity against pathogens. [3] 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. [4] 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. [5]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 67 mg/mL
(198.6 mM)
Water Insoluble
Ethanol ''8 mg/mL

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.

30 mg/mL

Chemical Information

Molecular Weight 337.35
Formula

C16H20FN3O4

CAS No. 165800-03-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(=O)NCC1CN(C(=O)O1)C2=CC(=C(C=C2)N3CCOCC3)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05175794 Not yet recruiting Diagnostic Test: Xpert® MTB/XDR Drug Resistant Tuberculosis|MDR-TB|XDR-TB|Tuberculosis Centre for the AIDS Programme of Research in South Africa|KNCV Tuberculosis Foundation|Amsterdam Institute for Global Health and Development|Ospedale San Raffaele|Foundation for Innovative New Diagnostics Switzerland|National Institute for Medical Research Tanzania|University of St Andrews|Global Alliance for TB Drug Development|Wits Health Consortium (Pty) Ltd|Institute of Human Virology Nigeria|Ethiopian Public Health Institute February 1 2022 --
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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

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.

Handling Instructions

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