Eravacycline dihydrochloride (TP-434 dihydrochloride) is a potent and broad-spectrum antibacterial agent.
性状
Solid
体外研究(In Vitro)
Eravacycline is potent antibiotic against A. baumannii , including isolates that are resistant to sulbactam, SM 7338, and BAY 41-6551. Eravacycline shows greater activity than BAY 41-6551, and colistin. The eravacycline MIC50/90 values are 0.5/1 mg/L. Eravacycline shows inhibitory effects on six E. coli with MICs ranging from 0.125 to 0.25 mg/L. Eravacycline dihydrochloride is a synthetic antibiotic, with inhibits bacterial protein synthesis through binding to the 30S ribosomal subunit. Eravacycline displays broad spectrum activity against gram-negative bacteria in the panel except P. aeruginosa , as well as excellent activity against major gram-positive pathogens, including methicillin-resistant S. aureus . Eravacycline also displays potent ribosomal inhibition. Eravacycline shows potent broad-spectrum activity against 90% of the isola
体内研究(In Vivo)
Mice are treated with two-fold increasing doses (range 3.125 to 50 mg/kg) of eravacycline every 12 hours. The mean fAUC/MIC magnitude associated with net stasis and 1-log kill endpoint are 27.97 ± 8.29 and 32.60 ± 10.85, respectively. Eravacycline is active in multiple murine models of infection against clinically important Gram-positive and Gram-negative pathogens. Eravacycline is efficacious in mouse septicemia models, demonstrating 50% protective dose values of ≤1 mg/kg of body weight once a day (q.d.) against Staphylococcus aureus. The PD 50 values against Escherichia coli isolates are 1.2 to 4.4 mg/kg q.d. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-80°C, protect from light, stored under nitrogen 该产品在溶液状态不稳定,建议您现用现配,即刻使用。
ClinicalTrial
参考文献
[1]. Seifert H, et al. In-vitro activity of the novel fluorocycline eravacycline against carbapenem non-susceptible Acinetobacter baumannii. Int J Antimicrob Agents. 2017 Jul 10.[2]. Zhao M, et al. In Vivo Pharmacodynamic Target Assessment of Eravacycline against Escherichia coli in a Murine Thigh Infection Model. Antimicrob Agents Chemother. 2017 Jun 27;61(7).
溶解度数据
In Vitro: H2O : 50 mg/mL (79.18 mM; Need ultrasonic)DMSO : ≥ 50 mg/mL (79.18 mM)