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Eperezolid
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Eperezolid图片
CAS NO:165800-04-4
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Eperezolid(PNU-100592) 是一种恶唑烷酮类抗菌剂,无论甲氧西林对葡萄球菌的敏感性如何(MIC90= 1-4 mg/ml),Eperezolid 都表现出良好的体外抑制活性。
Cas No.165800-04-4
别名N-[[(5S)-3-[3-氟-4-[4-(2-羟基乙酰基)-1-哌嗪基]苯基]-2-氧代-5-噁唑烷基]甲基]-乙酰胺,PNU-100592
化学名N-[[(5S)-3-[3-fluoro-4-[4-(2-hydroxyacetyl)piperazin-1-yl]phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl]acetamide
Canonical SMILESCC(=O)NCC1CN(C(=O)O1)C2=CC(=C(C=C2)N3CCN(CC3)C(=O)CO)F
分子式C18H23FN4O5
分子量394.4
溶解度≥ 14.05mg/mL in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

MIC50: 0.5, 1.0, 2.0, 1.0, 16.0 and 2.0 mg/L for Pcptostreptococcus, Propionibacterium acnes, Ciostridium pefringens, Clostridium dijiicile, Bactrroidesjagilis, and Fusobacterium, respectivley

Anaerobic bacteria are a common cause of serious infections. Anaerobic species which predominate in clinical infections include the Bacteroides fragilis group, Clostridium spp. and Peptostreptococcus spp. The oxazolidinones are a novel class of synthetic antimicrobials inhibiting the initiation of protein synthesis. Two compounds of this class, eperezolid and linezolid have been shown to inhibit Enterococcus faecalis and Enterococcus faecium.

In vitro: Ninety per cent of all tested Propionibacterium acnes (30 strains), PeptostreptococccuJ spp. (50 strains), C. perjringens (50 strains) and C. dficile (50 strains) were inhibited by<2 mg/L eperezolid. Linezolid showed higher activity (MIC90 4.0 mg/L) against B. jragilis (100 strains) compared to eperezolid (MIC90 16 mg/L) [1].

In vivo: The in vivo effectiveness of eperezolid and linezolid against one strain each of Enterococcus faecalis and vancomycin-resistant Enterococcus faecium was examined in a rat intraabdominal abscess model. Eperezolid was ineffective at doses of 25 mg/kg of body weight twice daily for the reductions in abscess bacterial density for E. faecalis. Against E. faecium infections, intravenous eperezolid was effective, reducing densities approximately 2 log10 CFU/g [2].

Clinical trials: Oral administration of eperezolid (1 000 mg PO) to healthy volunteers has earlier been reported to yield peak serum concentration of 6.28 mg/L, respectively, while the trough concentration was estimated to be 1.62 mg/L, respectively [3].

References:
[1] Edlund C, Oh H, Nord CE.  In vitro activity of linezolid and eperezolid against anaerobic bacteria. Clin Microbiol Infect. 1999;5(1):51-53.
[2] Schülin T, Thauvin-Eliopoulos C, Moellering RC Jr, Eliopoulos GM.  Activities of the oxazolidinones linezolid and eperezolid in experimental intra-abdominal abscess due to Enterococcus faecalis or vancomycin-resistant Enterococcus faecium. Antimicrob Agents Chemother. 1999;43(12):2873-6.
[3] Schaadt RD, Batts DH, Daley-Yates PT, Pawsey SD, Stalker DJ, Zurenko GE.   Serum inhibitory titers and serum bactericidal titers for human subjects receiving multiple doses of the antibacterial oxazolidinones eperezolid and linezolid. Diagn Microbiol Infect Dis. 1997;28(4):201-4.