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MCE 国际站:Ceftaroline fosamil
中文名:头孢洛林酯
CAS:400827-46-5
品牌:MedChemExpress (MCE)
存储条件:-20°C, sealed storage, away from moisture
生物活性:Ceftaroline fosamil (TAK-599) 是一种头孢菌素衍生物,是抗甲氧西林耐药 金黄色葡萄球菌 (MRSA) T-91825 的 N-膦酰基前药。 Ceftaroline fosamil可用于MRSA感染的研究[1][2][3]。
体内:Ceftaroline fosamil (sc) 显示出对 S 引起的实验性全身感染的保护作用。 aureus N133 在小鼠体内,ED50 为 1.60-2.37 mg/kg[1]。Ceftaroline fosamil (10 mg/kg; sc)在大鼠和猴子的血液中迅速消失并顺利转化为T-91825[1]。
动物体内实验:使用中性粒细胞减少性肺部感染模型研究了 17 种临床金黄色葡萄球菌分离株(2 个 MSSA,15 个 MRSA)。接种后 3 小时开始,每组 6 只小鼠接受头孢洛林酯治疗 24 小时。头孢洛林酯剂量以 0.2 mL 皮下注射给药。对照动物以与治疗方案相同的体积、途径和频率施用生理盐水[1]。
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研究领域:Anti-infection
作用靶点:Bacterial | Antibiotic
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参考文献:[1]. Ishikawa T, et, al. TAK-599, a novel N-phosphono type prodrug of anti-MRSA cephalosporin T-91825: synthesis, physicochemical and pharmacological properties. Bioorg Med Chem. 2003 May 29;11(11):2427-37.
[2]. Jacqueline C, et, al. In vivo efficacy of ceftaroline (PPI-0903), a new broad-spectrum cephalosporin, compared with linezolid and vancomycin against methicillin-resistant and vancomycin-intermediate Staphylococcus aureus in a rabbit endocarditis model. Antimicrob Agents Chemother. 2007 Sep;51(9):3397-400.
[3]. Parish D, et, al. Ceftaroline fosamil, a cephalosporin derivative for the potential treatment of MRSA infection. Curr Opin Investig Drugs. 2008 Feb;9(2):201-9.
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