Linezolid (PNU-100766) - Moligand™, 10mM in DMSO , Bacterial 70S ribosome inhibitor, CAS No.165800-03-3, Bacterial 70S ribosome inhibitor

CAS: 165800-03-3 Cat. No.: L408943 Peso molecular: 337.35 Número EC: 605-416-1

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

(S)-N-((3-(3-fluoro-4-morpholinophenyl)-2-oxooxazolidin-5-yl)methyl)acetamide

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

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. Linezolid is a potent inhibitor of cell-free transcription-translation in E. coli, exhibiting 50% inhibitory concentrations (IC50s) of 1.8 mM. Linezolid\xa0is an oxazolidinone, a new class of antibacterial agents with enhanced activity\xa0against\xa0pathogens. 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.

In vivo

Cell Data

cell lines：U87, LN229, NIH3T3, HUVECs, BaF3 and TT thyroid carcinoma cells

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Sinónimos

(S)-N-((3-(3-fluoro-4-morpholinophenyl)-2-oxooxazolidin-5-yl)methyl)acetamide

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

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

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Grado

Moligand™

Tipo de acción

INHIBITOR

Mecanismo de acción

Bacterial 70S ribosome inhibitor

Propiedades del producto

• ALogP: 0.7

Nombres e identificadores

• Isómeros SMILES: CC(=O)NC[C@H]1CN(C(=O)O1)C2=CC(=C(C=C2)N3CCOCC3)F
• WGK Alemania: 3
• RTECS: AC2720000
• Peso molecular: 337.35
• Reaxy-Rn: 9426017
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=9426017&ln=

Objetivos asociados (humanos)

MAOB Tclin Amine oxidase [flavin-containing] B (0 Activities)

Discover Target: MAOB

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MAOA Tclin Amine oxidase [flavin-containing] A (0 Activities)

Discover Target: MAOA

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propiedades químicas y físicas

• Punto de fusión (°C): 179 °C

Referencias

1. Chong-Fa Lai, Wei-Bin Xiao, Hua-Cheng Yan, Hui Yang, Lu-Xia Wang, Hui Guan, Qiu-ju Peng, Zhi-Rong Deng, Jian-Wen Chen, Lin-Kun An, Lei Shi.  (2020)  ZTW-41, a Potent Indolizinoquinoline-5,12-Dione Derivative Against Drug-Resistant Staphylococci and Enterococci Bacteria.  Microbial Drug Resistance,  26  (2): (100-109).  [PMID:31441704] [10.1089/mdr.2019.0008]

2. Tingting Liu, Xiaomin Chen, Guanxuanzi Zhang, Jing Zhao, Qian Lu, Fang Wang, Hongxia Li, Bing Liu, Ping Zhu.  (2024)  An LCMS/MS method for the simultaneous determination of ten antimicrobials and its application in critically ill patients.  JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS,      [PMID:39357099] [10.1016/j.jpba.2024.116489]

3. Shuai Dong, Xingyuan Bai, Bin Chen, Minzhe Fan, Qi Liu, Yubo Zhao, Linsen Li*, Dan Zhu.  (2025)  Panzerina lanata accelerates methicillin-resistant Staphylococcus aureus eradication by promoting migration and activation of neutrophils.  Frontiers in Pharmacology,      [PMID:39877391] [10.3389/fphar.2024.1501744]

4. Jinyao Liu, Yingying Pang, Wenyan Li, Juanjuan Sun, Yujie He, Yonghong Guo, Jing Dong.  (2025)  Impact of hepatic impairment and renal failure on the pharmacokinetics of linezolid and its metabolites: contribution of hepatic metabolism and renal excretion.  ANTIMICROBIAL AGENTS AND CHEMOTHERAPY,      [PMID:40227039] [10.1128/aac.01892-24]

5. Jin-yao Liu, Ying-ying Pang, Piao-piao Wang, Wen-yan Li, Jing Dong.  (2025)  Validated HPLC Method for the Pharmacokinetic Study of Linezolid in Rats.  BIOMEDICAL CHROMATOGRAPHY,  39  (7): (e70107).  [PMID:40384292] [10.1002/bmc.70107]

6. Tianmeng Li, Hong Shen, Peng Wang, Yu Wang, Jun Liu, Meibo He, Li Gu, Shuai Wang, Ming Wei.  (2025)  Antibiofilm activity of arachidonic acid against linezolid-resistant Enterococcus faecalis: A potential strategy for combating biofilm-related infections.  MICROBIAL PATHOGENESIS,      [PMID:40287107] [10.1016/j.micpath.2025.107629]

7. Chen Huang, Ling-Jie Guo, Jia-Yi Li, Yue-Wen Chen, Bing Wu, Yi-Wei Liu, Chen-Zhi Zhang, Wei-Wei Lin, Ye Yang, Jin-Yuan Chen, Zhou-Jie Liu.  (2025)  A CRISPR-Cas12a Fluorescent Aptasensor for Point-of-Care Drug Concentration Detection: A Synergistic Regulation by DNA Aptamer and RNA Blocker.  ANALYTICAL CHEMISTRY,      [PMID:41144643] [10.1021/acs.analchem.5c03744]

8. Jian-Guo Li, Wei-Cheng Zhong, Long-Gen Zhong, Chao-Yan Niu, Ting-Yin Lu, Chuan-Jian Zhang, Jian Sun, Xiao-Ping Liao, Yu-Feng Zhou.  (2025)  Auranofin potentiates linezolid activity against MRSA by disrupting redox homeostasis and inhibiting SarA-mediated virulence and biofilm.  Virulence,      [PMID:41400929] [10.1080/21505594.2025.2605759]

9. Yang Liu, Yan Lu, Weilian Bao, Haiyan Zhu, Guoqi Yuan, Linfeng Guo, Hong Li, Jiyang Li, Tong Wu, Xunlong Shi, Daofeng Chen.  (2026)  Quercitrin Inhibits NETosis via Histone H3 to Alleviate the Severity of Viral Pneumonia With Drug-Resistant Bacteria Co-Infection in Mice.  PHYTOTHERAPY RESEARCH,      [PMID:41520363] [10.1002/ptr.70190]