Gatifloxacin

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

第四代氟喹诺酮类抗生素，可抑制细菌 DNA 旋转酶和拓扑异构酶 IV。

A fourth-generation fluoroquinolone antibiotic that inhibits the bacterial DNA gyrase and topoisomerase IV; displays 2- to 16-fold more active than ciprofloxacin and ofloxacin against Staphylococcus aureus with MICs of 0.1-0.78 ug/mL.(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.

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.

Gatifloxacin (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.

AM 1155 | BMS 206584-01 | PD 135432 | AM1155 | BMS206584-01

GPCR/G Protein

Antibacterial

TopoIV

Infection

——

112811-59-3

375.3941

C19H22FN3O4

>98% (HPLC)

10 mM in DMSO

COC1=C2N(C=C(C(O)=O)C(=O)C2=CC(F)=C1N1CCNC(C)C1)C1CC1

3-Quinolinecarboxylic acid, 1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methyl-1-piperazinyl)-4-oxo-

(-20℃)

With Ice Pack

≥ 2 years