Gatifloxacin是一种具有广谱抗菌活性的氟喹诺酮类抗生素。它可抑制大肠杆菌 DNA 解旋酶 (IC50=0.109 μg/ml) 和细菌 II 型拓扑异构酶(IC50=13.8 μg/ml)。在动物模型中,它有抗细菌性结膜炎作用。
产品描述
Gatifloxacin is an antibiotic of the fourth-generation fluoroquinolone family, that like other members of that family, inhibits the bacterial enzymes DNA gyrase and topoisomerase IV.
体外活性
Gatifloxacin提高正常和糖尿病大鼠中血清肾上腺素浓度.Gatifloxacin减小正常和糖尿病大鼠的血清葡萄糖浓度.
体内活性
Gatifloxacin针对细菌II型拓扑异构酶显示有效的抑制活性,对金黄色葡萄球菌拓扑异构酶和肠杆菌DNA促旋酶的IC 50分别为13.8 mg/mL和0.109 mg/mL,对HeLa细胞拓扑异构酶II 的活性最低,IC 50 =265 mg/mL。Gatifloxacin抑制M. tuberculosis ATCC 35801,MIC为0.125 μg/mL。Gatifloxacin和Ciprofloxacinplus联用表现对19%的31种绿脓杆菌的协同作用。Gatifloxacin的活性低于ciprofloxacin的2倍,活性比ofloxacin对Enterobacteriaceae低2倍。Gatifloxacin对流感嗜血杆菌,军团菌,幽门螺杆菌有很强的抗菌活性(MIC90s,0.03-0.06 mg/L),有至少8倍的抗衣原体和抗支原体效力(加替沙星MIC90s,0.13 mg/L)。
Cas No.
112811-59-3
分子式
C19H22FN3O4
分子量
375.4
别名
BMS 206584-01;PD 135432;加替沙星;CG5501;AM-1155;BMS-206584
储存和溶解度
DMSO:3.8 mg/mL (10 mM)),with gentle warming
Powder: -20°C for 3 years
In solvent: -80°C for 2 years