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121577-32-0

中文名称 121577-32-0
英文名称 Gatifloxacinacid
CAS 121577-32-0
分子式 C19H22FN3O4.ClH
分子量 411.859
MOL 文件 121577-32-0.mol
121577-32-0 结构式 121577-32-0 结构式

基本信息

中文别名
加替沙星盐酸盐
1-环丙基-6-氟-8-甲氧基-7-(3-甲基哌嗪-1-基)-4-氧代-1,4-二氢喹啉-3-羧酸盐酸盐
英文别名
Gatifloxacinacid
AM 1155 hydrochloride
PD 135432 hydrochloride)
BMS-206584 (hydrochloride)
BMS 206584-01 hydrochloride
Gatifloxacin hydrochloride (AM 1155 hydrochloride
AM 1155 HYDROCHLORIDE
BMS 206584-01 HYDROCHLORIDE
PD 135432 HYDROCHLORIDE
3-Quinolinecarboxylicacid,1-cyclopropyl-6-fluoro-1,4-dihydro-8-Methoxy-7-(3-Methyl-1-piperazinyl)-4-oxo-,hydrochloride (1:1)
3-Quinolinecarboxylic acid, 1-cyclopropyl-6-fluoro-1,4-dihydro-8-Methoxy-7-(3-Methyl-1-piperazinyl)-4-oxo-, Monohydrochloride (9CI)
所属类别
分析化学:药典标准品和杂质标准品

物理化学性质

储存条件Inert atmosphere,2-8°C
溶解度溶于二甲基亚砜
形态粉末
颜色White to off-white

常见问题列表

生物活性
Gatifloxacin hydrochloride (AM-1155 hydrochloride) 是一种有效的氟喹诺酮类抗生素 (antibiotic),具有广谱抗菌活性。Gatifloxacin hydrochloride (AM-1155 hydrochloride) 可抑制细菌 II 型拓扑异构酶 (type II topoisomerases) (IC50=13.8 μg/ml; 金黄色葡萄球菌拓扑异构酶 IV) 和大肠杆菌 DNA 解旋酶 (IC50=0.109 μg/ml)。Gatifloxacin hydrochloride (AM-1155 hydrochloride) 在动物模型中,可用于细菌性结膜炎的研究。
靶点

Topoisomerase II

36.7 μM ()

体外研究

Gatifloxacin hydrochloride is against S. aureus MS5935 topoisomerase IV, E. coli NIHJ JC-2 DNA gyrase and HeLa cell topoisomerase II with IC 50 values of 13.8 μg/ml, 0.109 μg/ml, and 265 μg/ml, respectively.Gatifloxacin hydrochloride is against S. aureus MS5935 topoisomerase IV, E. coli NIHJ JC-2 DNA gyrase and HeLa cell topoisomerase II with MIC values of 0.05 μg/ml, 0.0063 μg/ml, and 122 μg/ml, respectively.Gatifloxacin hydrochloride exhibits antibacterial activities for wild-type strains (MS5935, MS5952, MR5867 and MR6009) the first-, second-, third-, and fourth-step mutants with MIC values of 0.05 to 0.10 μg/ml, 0.20 μg/ml, 1.56 to 3.13 μg/ml, 1.56 to 6.25 μg/ml, and 50 to 200 μg/ml, respectively. Gatifloxacin hydrochloride displays the most potent activity against the second- and third-step mutants (MS5952, MR5867 and MR6009) except for the second-step mutant of strain MS5935.Gatifloxacin hydrochloride has potent activity against norA transformant NY12 (MIC, 0.39 μg/ml).Gatifloxacin hydrochloride (20-100 μM; 72 hours) significantly decreases insulin content to 60% at Day 1, and continues to be reduced to 50.1% and 44.7% at Day 3 by 20 μM and 100 μM Gatifloxacin hydrochloride, respectively.

体内研究

Gatifloxacin hydrochloride (subcutaneous injection; 100 mg/kg; 3 times a day; 30 days) significantly decreases the number of lesions in mouse footpad with Nocardia brasiliensis .

Animal Model: Female BALB/c mice with Nocardia brasiliensis in the right hind footpad
Dosage: 100 mg/kg
Administration: Subcutaneous injection; 3 times a day; 30 days
Result: Reduced the production of lesions in mice.
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