| CAS |
No.1334714-66-7 |
| 英文名称 |
Eravacycline dihydrochloride |
| 别名 |
;TP-434dihydrochloride;TP-434-046;AC-LYSINE; |
| 分子式 |
C27H33Cl2FN4O8 |
| 分子量 |
631.48 |
| 溶解性 |
Soluble in Water |
| 纯度 |
≥98% |
| 外观(性状) |
Solid |
| 储存条件 |
Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| 运输条件 |
冷藏运输 |
| SMILES |
CN(C)[C@H]1[C@@H]2C[C@@H]3CC4=C(C=C(C(=C4C(=C3C(=O)[C@@]2(C(=C(C1=O)C(=O)N)O)O)O)O)NC(=O)CN5CCCC5)F.Cl.Cl |
| 靶点 |
Bacterial |
| 通路 |
Anti-infection |
| 背景说明 |
是一种有效的广谱抗菌化合物。 |
| 生物活性 |
Eravacycline dihydrochloride (TP-434 dihydrochloride) is a potent and broad-spectrum antibacterial agent.[1-5] |
| In Vitro |
Eravacycline dihydrochloride 是针对鲍曼不动杆菌的有效抗生素，包括对舒巴坦、SM 7338 和 BAY 41-6551 耐药的菌株。Eravacycline dihydrochloride 显示出比 BAY 41-6551 和多粘菌素更高的活性。Eravacycline dihydrochloride MIC50/90 值为 0.5/1 mg/L[1]。Eravacycline dihydrochloride 对 6 种大肠杆菌具有抑制作用，MIC 范围为 0.125 至 0.25 mg/L[2]。Eravacycline dihydrochloride 是一种合成抗生素，通过与 30S 核糖体亚基结合来抑制细菌蛋白质的合成。Eravacycline dihydrochloride 对除铜绿假单胞菌外的革兰氏阴性菌表现出广谱活性，以及对主要革兰氏阳性病原体的出色活性，包括耐甲氧西林金黄色葡萄球菌。Eravacycline dihydrochloride 还表现出有效的核糖体抑制作用[3]。Eravacycline dihydrochloride 对每个组中 90% 的分离株 (MIC90) 显示出有效的广谱活性，浓度范围为 ≤0.008 至 2 μg/mL，对于除 Pseudomonas aeruginosa 以外的所有物种组和 Burkholderia cenocepacia ((MIC90 均为 32 μg/mL)。Eravacycline dihydrochloride 对多重耐药细菌具有活性，包括那些表达超广谱 β-内酰胺酶的细菌和赋予对其他类别抗生素耐药性的机制，包括碳青霉烯耐药性[4]。 |
| In Vivo |
Eravacycline dihydrochloride 在针对临床上重要的革兰氏阳性和革兰氏阴性病原体的多种小鼠感染模型中具有活性。Eravacycline dihydrochloride 在小鼠败血症模型中有效，证明每天一次 (qd) ≤ 1 mg/kg 体重对金黄色葡萄球菌的 50% 保护剂量值。对大肠杆菌分离株的 PD50 值为 1.2 至 4.4 mg/kg qd[5]。 |
| 动物实验 |
Rats: Pharmacokinetic (PK) parameters are determined in Sprague?Dawley rats. Animals are fasted overnight (minimum of 12 h) and given a single oral (10 mg/kg) or IV dose (1 mg/kg) of eravacycline followed by a sampling scheme for 24 h. Plasma and dosing solution concentrations are determined by TurboIonspray LC/MSMS analysis using appropriate standard curves. PK parameters are calculated by noncompartmental analysis[3]. Mice: Eravacycline is formulated in sterile 0.9% saline. BALB/c mice are inoculated with 0.2 mL of prepared bacterial inoculum via intravenous injection to seed the kidney. Animals are administered antibiotics (eravacycline) at 10 ml/kg i.v. via the tail vein 12 and 24 h postinfection. Then the bacterial burden is determined[5]. |
| 数据来源文献 |
[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. |
| 规格 |
1mg 5mg |
| 单位 |
瓶 |
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