Linezolid (PNU-100766)

Catalog No.S1408 Batch:S140803

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Technical Data

Formula

C16H20FN3O4
Molecular Weight 337.35 CAS No. 165800-03-3
Solubility (25°C)* In vitro DMSO 68 mg/mL (201.57 mM)
Ethanol 10 mg/mL (29.64 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
30%PEG400 0.5%Tween80 5%propylene glycol
30.0mg/ml Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified PEG400 stock solution to 5 μL of Tween80, mix evenly to clarify it; add 50 μL Propylene glycol to the above system, mix evenly to clarify it; then continue to add 645 μL ddH2O to adjust the volume. to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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)

Customer Product Validation

Data from [Antimicrob Agents Chemother, 2014, 58(7), 4113-22]

Data from [Data independently produced by , , Sci Rep, 2016, 6:22571]

Data from [Data independently produced by , , Int J Antimicrob Agents, 2016, 47(3):195-201]

Data from [Data independently produced by , , Front Microbiol, 2018, 9:1175]

Selleck's Linezolid (PNU-100766) has been cited by 23 publications

Assessment of Lipophilicity Parameters of Antimicrobial and Immunosuppressive Compounds [ Molecules, 2023, 28(6)2820] PubMed: 36985792
Assessment of Lipophilicity Parameters of Antimicrobial and Immunosuppressive Compounds [ Molecules, 2023, 28(6), 2820] PubMed: None
Efficacy of a Novel Antibacterial Agent Exeporfinium Chloride, (XF-73), Against Antibiotic-Resistant Bacteria in Mouse Superficial Skin Infection Models [ Infect Drug Resist, 2023, 16:4867-4879] PubMed: 37520450
Efficacy of a Novel Antibacterial Agent Exeporfinium Chloride, (XF-73), Against Antibiotic-Resistant Bacteria in Mouse Superficial Skin Infection Models [ Infect Drug Resist, 2023, 16:4867-4879] PubMed: 37520450
Impaired Succinate Oxidation Prevents Growth and Influences Drug Susceptibility in Mycobacterium tuberculosis [ mBio, 2022, 13(4):e0167222] PubMed: 35856639
Mechanism underlying linezolid-induced peripheral neuropathy in multidrug-resistant tuberculosis [ Front Pharmacol, 2022, 13:946058] PubMed: 36160387
Activity of Drug Combinations against Mycobacterium abscessus Grown in Aerobic and Hypoxic Conditions [ Microorganisms, 2022, 10(7)1421] PubMed: 35889140
Anti-staphylococcus Antibiotics Interfere With the Transcription of Leucocidin ED Gene in Staphylococcus aureus Strain Newman. [ Front Microbiol, 2020, 11:265] PubMed: 32194524
Mitochondrial ROS promote macrophage pyroptosis by inducing GSDMD oxidation. [ J Mol Cell Biol, 2019,  pii: mjz020] PubMed: 30860577
A rapid, low pH, nutrient stress, assay to determine the bactericidal activity of compounds against non-replicating Mycobacterium tuberculosis. [ PLoS One, 2019, 14(10):e0222970] PubMed: 31589621

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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