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%
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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.
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基本信息 | |
别名 |
Pretomanid;(S)-PA 824
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可溶性/溶解性 |
Ethanol :16mg/mL(44.53mM)
DMSO :72mg/ml(200.41 mM) |
生物活性 | |
靶点 |
tuberculosis
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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).
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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.
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参考文献 | |
参考文献 |
PA-824 exhibits time-dependent activity in a murine model of tuberculosis.
Ahmad Z,et al. Antimicrob Agents Chemother. 2011 Jan;55(1):239-45. PMID: 20937781 䔸Żᩄ 族痛셌Ų 族痛셌Ų Item 褐 Count ๏ 趌๐ 侮靴 ᠠi S ñ ñ 眘⮦眀⮦敲痛๏ࠃ 馸鳘祖Item ƞƞ Count 洣盜᬴叫㺍痭ᠠ靴i 縉 靴蘿敌ଧ靴ᠠi ᭰叫㺍痭ᡸ顴먲ନ魈 鸤�ଭ鶔 懲 랖ନҸ 煮 ﭬz�ଭ鶔 삲W鸤 ᨼĊ 煮 섈W豈勤섫W豈́煮ﭬz 섪W섲Ẃ |
分子结构图