121577-32-0
- CAS号:121577-32-0
- 英文名:Gatifloxacinacid
- 中文名:121577-32-0
- CBNumber:CB11074612
- 分子式:C19H22FN3O4.ClH
- 分子量:411.859
- MOL File:121577-32-0.mol
- 储存条件 :under inert gas (nitrogen or Argon) at 2-8°C
- 溶解度 :Soluble in DMSO
- 形态 :Powder
- 颜色 :White to off-white
121577-32-0性质、用途与生产工艺
- 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。
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靶点
Topoisomerase II
36.7 μM ()
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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.
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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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- 国家:印度
- 产品数:6100
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