加替沙星作用机制 - Medchemexpress - MCE中国

1、Product Data SheetGatifloxacinCat. No.: HY-10581CAS No.: 112811-59-3分式: CHFNO分量: 375.39作靶点: Bacterial; Topoisomerase作通路: Anti-infection; Cell Cycle/DNA Damage储存式: 4C, stored under nitrogen* In solvent : -80C, 6 months; -20C, 1 month (stored under nitrogen)溶解性数据体外实验 DMSO : 2 mg/mL (5.33 mM; Need ultr

2、asonic)H2O : 1 mg/mL (2.66 mM; Need ultrasonic)SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 2.6639 mL 13.3195 mL 26.6390 mL5 mM 0.5328 mL 2.6639 mL 5.3278 mL10 mM 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month (stored under nitrogen)。-80C 储存时，请在 6

3、个内使，-20C 储存时，请在 1 个内使。BIOLOGICAL ACTIVITY物活性 Gatifloxacin (AM-1155; BMS-206584; PD135432)种有效的氟喹诺酮类抗素 (antibiotic)，具有谱抗菌活性。Gatifloxacin 可抑制细 II 型拓扑异构酶 (type II topoisomerases) (IC50=13.8 g/ml; 葡萄球菌拓扑异构酶 IV) 和肠杆 DNA 解旋酶 (IC50=0.109 g/ml)。Gatifloxacin 在动物模型中，可于治疗细菌性结膜炎。IC & Target Topoisomerase II36.7

4、M (IC50)体外研究Gatifloxacin is against S. aureus MS5935 topoisomerase IV, E. coli NIHJ JC-2 DNA gyrase and HeLa cell topoisomeraseII with IC50 values of 13.8 g/ml, 0.109 g/ml, and 265 g/ml, respectively1.Gatifloxacin is against S. aureus MS5935 topoisomerase IV, E. coli NIHJ JC-2 DNA gyrase and HeLa ce

5、ll topoisomeraseII with MIC values of 0.05 g/ml, 0.0063 g/ml, and 122 g/ml, respectively1.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 g/ml, 0.20 g/ml, 1.56

6、 to 3.13 g/ml, 1.56 toPage 1 of 2 www.MedChemE6.25 g/ml, and 50 to 200 g/ml, respectively. Gatifloxacin displays the most potent activity against the second- andthird-step mutants (MS5952, MR5867 and MR6009) except for the second-step mutant of strain MS59352.Gatifloxacin has potent activity against

7、 norA transformant NY12 (MIC, 0.39 g/ml)2.Gatifloxacin (20-100 M; 72 hours) significantly decreases insulin content to 60% at Day 1, and continues to bereduced to 50.1% and 44.7% at Day 3 by 20 M and 100 M gatifloxacin, respectively3.体内研究 Gatifloxacin (subcutaneous injection; 100 mg/kg; 3 times a da

8、y; 30 days) significantly decreases the number of lesionsin mouse footpad with Nocardia brasiliensis4.Animal Model: Female BALB/c mice with Nocardia brasiliensis in the right hind footpad.Dosage: 100 mg/kgAdministration: Subcutaneous injection; 3 times a day; 30 daysResult: Reduced the production of

9、 lesions in mice.户使本产品发表的科研献 Patent. US20180263995A1.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Takei M, et al. Inhibitory activities of gatifloxacin (AM-1155), a newly developed fluoroquinolone, against bacterial and mammalian type IItopoisomerases.Antimicrob A

10、gents Chemother. 1998 Oct;42(10):2678-81.2. Fukuda H, et al. Antibacterial activity of gatifloxacin (AM-1155, CG5501, BMS-206584), a newly developed fluoroquinolone, against sequentially acquiredquinolone-resistant mutants and the norA transformant of Staphylococcus aureus. Antimicrob Agents Chemother. 1998 Aug;42(8):1917-22.3. Yamada C, et al. Gatifloxacin acutely stimulates insulin secretion and chronically suppresses insulin biosynthesis. Eur J Pharmacol. 2006 Dec 28;553(1-3):67-72. Epub 2006 Sep 28.McePdfHeightCaution: Product has not been fully validated for