中文名:硫酸安普霉素
CAS:65710-07-8
品牌:MedChemExpress (MCE)
存储条件:4°C, sealed storage, away from moisture
生物活性:Apramycin sulfate 是一种氨基糖苷类抗生素,由 Streptomyces tenebrarius 菌株产生,用于兽医实践。
体外:Apramycin (4 mg/L) 抑制 99% 的肺炎克雷伯氏菌和 93% 的肠杆菌临床分离株。Apramycin (8 mg/L) 抑制 99% 的大肠杆菌、98% 的弗氏柠檬酸杆菌、96% 的普罗威登斯菌、92% 的黏质沙雷菌、97% 的摩氏摩根氏菌和 100% 的变形杆菌临床分离株,表现出显著优于临床标准氨基糖苷类抗生素 Gentamicin 和 Amikacin 的抗菌活性[1]。 Apramycin (100 μM, 10 min) 在 pH 由 7.3 降至 5.7 时在大肠杆菌中的胞质摄取量减少 11%,而 Gentamicin 和 Amikacin 的胞质摄取量分别减少 62% 和 51%[3]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内:Apramycin (200 mg/kg/d, s.c., 9 d) 在低剂量结核分歧杆菌气溶胶感染模型 IFN-γ 敲除小鼠的肺部显示出显著的体内疗效[2]。 Apramycin (16, 32, 80 mg/kg, s.c., 24 h) 在金黄色葡萄球菌败血症的中性粒细胞减少小鼠模型中剂量依赖性地减少肾脏中 2-5 log10 和血液中 2-3 log10 的细菌负荷[2]。 Apramycin (50 mg/kg/d, s.c., 21 d) 产生与 Gentamicin (10 mg/kg/d) 相等的肾毒性评分[3]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: M. tuberculosis low-dose aerosol infection model of IFN-γ knockout mice [2] Dosage: 200 mg/kg/d Administration: Subcutaneousinjection (s.c.) for 9 d Result: Showed a 2.4-log10 CFU reduction and better antituberculous activity compared to Amikacin (1.8-log10 reduction). Clinical Trial
参考详情:Apramycin sulfate (EBL 1003,硫酸安普霉素) - 仅供科研 | 抗生素 | MCE
参考文献:
[1]. Juhas M, et al. In vitro activity of apramycin against multidrug-, carbapenem- and aminoglycoside-resistant Enterobacteriaceae and Acinetobacter baumannii. J Antimicrob Chemother. 2019;74(4):944-952.
[2]. Meyer M, et al. In vivo efficacy of apramycin in murine infection models. Antimicrob Agents Chemother. 2014 Nov;58(11):6938-41.
[3]. Becker K, et al. Antibacterial activity of apramycin at acidic pH warrants wide therapeutic window in the treatment of complicated urinary tract infections and acute pyelonephritis. EBioMedicine. 2021 Nov;73:103652.