Linezolid (PNU-100766)

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

Linezolid (PNU-100766) Chemical Structure

Linezolid (PNU-100766) Chemical Structure

CAS: 165800-03-3

Selleck's Linezolid (PNU-100766) has been cited by 22 Publications

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Purity & Quality Control

Batch: Purity: 99.99%
99.99

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Biological Activity

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

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05944445 Recruiting Thrombocytopenia; Drugs Helwan University July 13 2023 --
NCT05571722 Not yet recruiting Antibiotic Prophylaxis|General Surgery Assistance Publique Hopitaux De Marseille April 3 2023 Phase 4
NCT05381194 Not yet recruiting Pre-XDR-TB Asan Medical Center|Funded by Korea Disease Control and Prevent Agency|Masan National Tuberculosis Hospital|Pusan National University Hospital|Samsung Medical Center|Seoul National University Hospital|Severance Hospital|Chonnam National University Hospital|International Tuberculosis Research Center|Investigational drug(Pretomanid) supported by Viatris Pharmaceutical August 1 2022 Phase 4
NCT05801484 Recruiting Side-effect of Antibiotic|Efficacy|Pharmacokinetics|Critical Illness|Intensive Care Unit ICU Cluj Municipal Clinical Hospital|Iuliu Hatieganu University of Medicine and Pharmacy July 1 2022 Not Applicable
NCT05175794 Recruiting 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 May 26 2022 --

Chemical lnformation & Solubility

Molecular Weight 337.35 Formula

C16H20FN3O4

CAS No. 165800-03-3 SDF Download Linezolid (PNU-100766) SDF
Smiles CC(=O)NCC1CN(C(=O)O1)C2=CC(=C(C=C2)N3CCOCC3)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 68 mg/mL ( (201.57 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble


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In vivo
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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.

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