Linezolid (PNU-100766)

Catalog No.S1408 Batch:S1408

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Technical Data

Formula

C16H20FN3O4
Molecular Weight 337.35 CAS No. 165800-03-3
Solubility (25°C)* In vitro DMSO 67 mg/mL (198.6 mM)
Water Insoluble
Ethanol ''8 mg/mL
* <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.)

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Biological Activity

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

Linezolid (PNU-100766) inhibits initiation complex formation with either the 30S or the 70S ribosomal subunits from Escherichia coli. It inhibits complex formation with Staphylococcus aureus 70S tight-couple ribosomes. [1] This compound is a potent inhibitor of cell-free transcription-translation in E. coli, exhibiting 50% inhibitory concentrations (IC50s) of 1.8 mM. [2] It is an oxazolidinone, a new class of antibacterial agents with enhanced activity against pathogens. [3] Its 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. It entails mutation of the 23S rRNA that forms the binding site. [4] This compound is an oxazolidinone whose mechanism of action involves inhibition of protein synthesis at a very early stage. It 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. It shows excellent in vitro activity against all the strains tested (MICs ≤ 1 μg/ml), including those resistant to SIRE. [5]

Protocol (from reference)

References

  • https://pubmed.ncbi.nlm.nih.gov/9835522/
  • https://pubmed.ncbi.nlm.nih.gov/9333037/
  • https://pubmed.ncbi.nlm.nih.gov/10428937/
  • https://pubmed.ncbi.nlm.nih.gov/12730138/
  • https://pubmed.ncbi.nlm.nih.gov/12499228/

Customer Product Validation

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

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.

Data from [ , , Sci Rep, 2016, 6:22571 ]

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

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

Data from [ , , Front Microbiol, 2018, 9:1175 ]

Selleck's Linezolid (PNU-100766) Has Been Cited by 24 Publications

3D collagen high-throughput screen identifies drugs that induce epithelial polarity and enhance chemotherapy response in colorectal cancer [ Commun Biol, 2025, 8(1):1261] PubMed: 40847193
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

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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.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.