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S82886

Eravacycline dihydrochloride

源叶(MedMol) 96%
  • 英文名:
  • Eravacycline dihydrochloride
  • 别名:
  • TP-434 dihydrochloride; TP-434-046
  • CAS号:
  • 1334714-66-7
  • 分子式:
  • C27H33Cl2FN4O8
  • 分子量:
  • 631.4773232
  • 核磁/质谱:
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源叶(MedMol) S82886-5mg 96% ¥3800.00元 预计交期:2-3天 - - - EA 加入购物车
源叶(MedMol) S82886-10mg 96% ¥6800.00元 预计交期:2-3天 - - - EA 加入购物车
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  • 提示:详情请下载说明书。
  • 产品描述: Eravacycline dihydrochloride (TP-434 dihydrochloride) is a potent and broad-spectrum antibacterial agent.
  • 靶点: Bacterial;Antibacterial
  • 体外研究:
    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 isolates (MIC90) in each panel at concentrations ranging from ≤0.008 to 2 μg/mL for all species panels except those of Pseudomonas aeruginosa and Burkholderia cenocepacia ((MIC90) values of 32 μg/mL for both organisms). Eravacycline is active against multidrug-resistant bacteria, including those expressing extended-spectrum β-lactamases and mechanisms conferring resistance to other classes of antibiotics, including carbapenem resistance
  • 体内研究:
    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 PD50 values against Escherichia coli isolates are 1.2 to 4.4 mg/kg q.d
  • 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). 3. Xiao XY, et al. Fluorocyclines: a potent, broad spectrum antibacterial agent. J Med Chem. 2012 Jan 26;55(2):597-605. 4. Sutcliffe JA, et al. Antibacterial activity of eravacycline (TP-434), a novel fluorocycline, against hospital and community pathogens. Antimicrob Agents Chemother. 2013 Nov;57(11):5548-58. 5. Grossman TH, et al. Eravacycline (TP-434) is efficacious in animal models of infection. Antimicrob Agents Chemother. 2015 May;59(5):2567-71.
  • 溶解性: Soluble  in  DMSO、H2O
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 1.584 ml 7.918 ml 15.836 ml
    5 mM 0.317 ml 1.584 ml 3.167 ml
    10 mM 0.158 ml 0.792 ml 1.584 ml
    50 mM 0.032 ml 0.158 ml 0.317 ml
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