| 产品描述： | Eperezolid is an oxazolidinone antibacterial agent. Eperezolid showed well in vitro inhibitory activity, regardless of methicillin susceptibility for staphylococci(MIC90= 1-4 mg/ml). |
| 靶点： |
Antibacterial; Antibiotic |
| 体外研究： |
The specific binding of eperezolid is dose-dependent and is proportional to the ribosome concentrations. The binding of eperezolid to the ribosome is competitively inhibited by chloramphenicol and lincomycin. However, unlike chloramphenicol and lincomycin, eperezolid does not inhibit the puromycin reaction, indicating that the oxazolidinones have no effect on peptidyl transferase. Antibiotic Eperezolid binds specifically to the 50S ribosomal subunit of Escherichia coli. eperezolid was found to bind only to the 50S subunit, with similar affinity as to the 70S ribosome, and to have no affinity for the 30S subunit. |
| 体内研究： |
Eperezolid (25 mg/kg；静脉注射/口服；q12h；4.5 天) 在感染粪肠球菌大鼠的腹腔脓肿模型中，静脉注射途径可降低 Vancomycin 耐药屎肠球菌感染模型的脓肿细菌密度，而对粪肠球菌感染模型无显著抑制作用。 |
| 参考文献： |
1. Rybak MJ, et al. Comparative in vitro activities and postantibiotic effects of the oxazolidinone compounds eperezolid (PNU-100592) and linezolid (PNU-100766) versus vancomycin against Staphylococcus aureus, coagulase-negative staphylococci, Enterococcus f 2. Lin AH, et al. The oxazolidinone eperezolid binds to the 50S ribosomal subunit and competes with binding of chloramphenicol and lincomycin. Antimicrob Agents Chemother. 1997 Oct;41(10):2127-31. 3. Zhou CC, et al. 1H nuclear magnetic resonance study of oxazolidinone binding to bacterial ribosomes. Antimicrob Agents Chemother. 2002 Mar;46(3):625-9. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.535 ml |
12.677 ml |
25.355 ml |
| 5 mM |
0.507 ml |
2.535 ml |
5.071 ml |
| 10 mM |
0.254 ml |
1.268 ml |
2.535 ml |
| 50 mM |
0.051 ml |
0.254 ml |
0.507 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京