产品说明书

Linezolid

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Chemical Structure| 165800-03-3 同义名 : 利奈唑胺 ;PNU-100766
CAS号 : 165800-03-3
货号 : A360550
分子式 : C16H20FN3O4
纯度 : 98%
分子量 : 337.346
MDL号 : MFCD00937825
存储条件：

粉末 Keep in dark place,Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(311.25 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Linezolid is the first of a new class of antibacterial drugs, the oxazolidinones. It has inhibitory activity against a broad range of gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA), glycopeptide-intermediate S. aureus (GISA), vancomycin-resistant enterococci (VRE) and penicillin-resistant Streptococcus pneumoniae. The drug also shows activity against certain anaerobes, including Clostridium perfringens, C. difficile, Peptostreptococcus spp. and Bacteroidesfragilis[3]. Linezolid is bacteriostatic against most susceptible organisms but displays bactericidal activity against some strains of pneumococci, Bacteroides fragilis and C. perfringens. Moreover, linezolid 600 mg twice daily produced >85% clinical/microbiological cure in vancomycin-resistant enterococcal infections[4]. Linezolid inhibits bacterial growth by targeting bacterial ribosomes and by interfering with bacterial protein synthesis. Lactic acidosis is a rare, but potentially lethal, side effect of linezolid[5]. In addition, the incidence of vomiting, diarrhea, and thrombocytopenia in patients treated with linezolid is significantly higher than that with other treatments. Linezolid seems to be more effective than vancomycin for treating people with SSTIs (skin and soft tissue infections) [6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.96mL

0.59mL

0.30mL

14.82mL

2.96mL

1.48mL

29.64mL

5.93mL

2.96mL
参考文献

[1]Swaney SM, Aoki H, et al. The oxazolidinone linezolid inhibits initiation of protein synthesis in bacteria. Antimicrob Agents Chemother. 1998 Dec;42(12):3251-5.

[2]Shinabarger DL, Marotti KR, et al. Mechanism of action of oxazolidinones: effects of linezolid and eperezolid on translation reactions. Antimicrob Agents Chemother. 1997 Oct;41(10):2132-6.

[3]Perry CM, Jarvis B. Linezolid: a review of its use in the management of serious gram-positive infections [published correction appears in Drugs. 2003;63(19):2126]. Drugs. 2001;61(4):525–551

[4]Clemett D, Markham A. Linezolid. Drugs. 2000;59(4):815–828

[5]Santini A, Ronchi D, Garbellini M, Piga D, Protti A. Linezolid-induced lactic acidosis: the thin line between bacterial and mitochondrial ribosomes. Expert Opin Drug Saf. 2017;16(7):833–843

[6]Li Y, Xu W. Efficacy and safety of linezolid compared with other treatments for skin and soft tissue infections: a meta-analysis. Biosci Rep. 2018;38(1):BSR20171125. Published 2018 Feb 13