121577-32-0
| 中文名称 | 121577-32-0 |
|---|---|
| 中文同义词 | 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;化合物GARCINONE D |
| 英文名称 | Gatifloxacinacid |
| 英文同义词 | Gatifloxacinacid;3-Quinolinecarboxylic acid, 1-cyclopropyl-6-fluoro-1,4-dihydro-8-Methoxy-7-(3-Methyl-1-piperazinyl)-4-oxo-, Monohydrochloride (9CI);3-Quinolinecarboxylicacid,1-cyclopropyl-6-fluoro-1,4-dihydro-8-Methoxy-7-(3-Methyl-1-piperazinyl)-4-oxo-,hydrochloride (1:1);BMS 206584-01 hydrochloride;Gatifloxacin hydrochloride (AM 1155 hydrochloride;PD 135432 hydrochloride);AM 1155 hydrochloride;AM 1155 HYDROCHLORIDE;BMS 206584-01 HYDROCHLORIDE;PD 135432 HYDROCHLORIDE |
| CAS号 | 121577-32-0 |
| 分子式 | C19H22FN3O4.ClH |
| 分子量 | 411.859 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 121577-32-0.mol |
| 结构式 |  |
121577-32-0 性质
| 储存条件 | under inert gas (nitrogen or Argon) at 2-8°C |
|---|---|
| 溶解度 | 溶于二甲基亚砜 |
| 形态 | 粉末 |
| 颜色 | 白色至米白色 |
|
Topoisomerase II 36.7 μM () |
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.
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. |