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Gatifloxacin

CAS No. : 112811-59-3

MCE 国际站：Gatifloxacin

产品活性：Gatifloxacin (AM-1155) 是一种有效的氟喹诺酮类抗生素 (antibiotic)，具有广谱抗菌活性。Gatifloxacin 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 在动物模型中具有抗细菌性结膜炎作用。

研究领域：Anti-infection  |  Cell Cycle/DNA Damage

作用靶点：Bacterial  |  Topoisomerase  |  Antibiotic

In Vitro: Gatifloxacin is against S. aureus MS5935 topoisomerase IV, E. coli NIHJ JC-2 DNA gyrase and HeLa cell topoisomerase II with IC₅₀ values of 13.8 μg/ml, 0.109 μg/ml, and 265 μg/ml, respectively.
Gatifloxacin 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 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 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 has potent activity against norA transformant NY12 (MIC, 0.39 μg/ml).
Gatifloxacin (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, respectively.

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

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