Gatifloxacin hydrochloride是一种氟喹诺酮类抗生素,有广谱抗菌活性。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) 。它在动物模型中,可研究细菌性结膜炎。
产品描述
Gatifloxacin hydrochloride is an antibiotic of the fourth-generation fluoroquinolone family, which can inhibit the bacterial enzyme DNA rotase and topoisomerase IV.
体内活性
All eyes showed evidence of infection by 48 hours postinoculation with 36 of 41 eyes (87.8%) exhibiting moderate-to-severe keratitis. All eyes exhibited corneal healing by day 15, with no significant differences among groups. Three of 4 groups receiving gatifloxacin tended to have smaller fluorescein retention area scores than did the ciprofloxacin group. No eyes tested positive for Pseudomonas at the end of the study. No corneal precipitates were found following as many as 48 doses/day of gatifloxacin[1].
动物实验
Heptanol-induced corneal ulcers in New Zealand White rabbits (n = 41; 8 females/group) were inoculated with 10(6) CFU of Pseudomonas aeruginosa. Gatifloxacin 0.3% dosing varied among 4 groups with frequencies of 16-48 doses/day (days 1-2), 3-16 doses/day (days 3-7), and maintenance dosing of 3-4 doses/day (days 8-22). Ciprofloxacin 0.3% was administered as labeled for corneal ulcers, with 44 doses on day 1, 16 doses on day 2, and 4 doses/day on days 3-21[1]
Cas No.
121577-32-0
分子式
C19H23ClFN3O4
分子量
411.86
别名
AM-1155 (hydrochloride);加替沙星盐酸盐;PD135432 (hydrochloride);BMS-206584 (hydrochloride)
储存和溶解度
H2O:10 mg/mL (24.28 mM),Need ultrasonic
DMSO:5 mg/mL (12.14 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years