AU1235是金刚烷脲,是一种MmpL3抑制剂。结核分枝杆菌蛋白MmpL3在细胞壁合成中起重要作用,它影响海藻糖单支霉菌酸酯跨内膜转运。
产品描述
AU1235 is a Mycobacterium tuberculosis inhibitor.
体外活性
AU1235 has a MIC of 0.1 μg/mL (0.3 μM) (minimum bactericidal concentration of 0.1 μg/mL. AU1235 is similarly active against MDR clinical isolates of M. tb displaying resistance to isoniazid, rifampicin, and pyrazinamide in addition to streptomycin, fluoroquinolones and/or ethambutol. AU1235 also inhibits Mycobacterium smegmatis and Mycobacterium fortuitum (MICs: 3.2 to 6.4 μg/mL). AU1235 (10 times MIC) does not increase the killing effect within the first 7 days indicating that the killing is time-dependent rather than concentration-dependent. In an anaerobic model involving non-replicating M. tb H37Rv bacilli, AU1235 at 10 μg/mL shows no detectable activity suggesting that it acts on a biosynthetic pathway required for active bacterial multiplication. AU1235 does not inhibit the biosynthesis of mycolic acids per se but specifically their ability to be transferred onto their cell wall and outer membrane acceptors.
Cas No.
1338780-86-1
分子式
C17H19F3N2O
分子量
324.34
储存和溶解度
DMSO:24 mg/mL (74 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years