PA-824

PA-824CAS号: 187235-37-6分子式: C14H12F3N3O5分子量: 359.26描述纯度储存/保存方法别名可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)参考文献

产品描述
描述

PA-824是一种抗肺结核药,作用于tuberculosis(肺结核),MIC低于2.8 μM。

纯度
98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
别名
Pretomanid;(S)-PA 824
可溶性/溶解性
Ethanol :16mg/mL(44.53mM)
DMSO :72mg/ml(200.41 mM)
生物活性
靶点
tuberculosis
In vitro(体外研究)
In vitro, PA-824 exhibits the high activity against multidrug-resistant clinical isolates from Asia (India and South Korea) and from throughout the United States (MIC A recent study shows that single-nucleotide polymorphisms of PA-824 resistance genes (fgd1 and ddn ) don’t significantly affect the PA-824 MICs (≤ 0.25 μg/ml).
In vivo(体内研究)
In the rapid tuberculosis mouse model, PA-824 shows significant anti-microbial activity in a dose-dependent manner: at 50 mg/kg, PA-824 in MC produces a more than 1-log reduction of the CFU in the lungs; at 100 mg/kg it produces about a 2-log reduction, and at 300 mg/kg it produces a 3-log reduction. Furthermore, long-term treatment of PA-824 at 100 mg/kg in cyclodextrin/lecithin also leads to the reduction of the bacterial load below 500 CFU in the lungs and spleen. PA-824 exhibits time-dependent anti-microbial activity in a murine model of tuberculosis with a maximal observed bactericidal effect of 0.1 log CFU/day over 24 days.
参考文献
参考文献
PA-824 exhibits time-dependent activity in a murine model of tuberculosis.
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分子结构图

PA-824