Catalog No.S1340 Synonyms: AM-1155, CG5501, BMS-206584
Molecular Weight(MW): 375.39
Gatifloxacin is an antibiotic of the fourth-generation fluoroquinolone family, and inhibits the bacterial enzymes DNA gyrase and topoisomerase IV.
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Cleavable complex formation with nuclear DNA in P. falciparum treated with topoisomerase poisons. Parasites were metabolically labeled with [3H]hypoxanthine, treated with etoposide (■), gatifloxacin (●), levofloxacin(▲), ciprofloxacin (□), fleroxacin (○), or nalidixic acid (△) at the indicated concentrations for 18-22 h, lysed with SDS and digested with RNases. SDS and protein-bound DNA were precipitated with potassium. The fold increase in nuclear DNA capture as compared to solvent controls (mean of triplicate determinations) was plotted against concentration. Coefficient of variation for each data point was 19%.
Biochem Pharmacol,2015, 95(4):227-237.. Gatifloxacin purchased from Selleck.
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|Description||Gatifloxacin is an antibiotic of the fourth-generation fluoroquinolone family, and inhibits the bacterial enzymes DNA gyrase and topoisomerase IV.|
Gatifloxacin has somewhat better in vitro activity against M. tuberculosis than moxifloxacin, and both are much more active than levofloxacin. Gatifloxacin is against M. tuberculosis ATCC 35801 with MICs of 0.125 μg/mL.  Gatifloxacin possesses potent inhibitory activities against bacterial type II topoisomerases (50% inhibitory concentration [IC50] = 13.8 mg/mL for S. aureus topoisomerase IV; IC50 = 0.109 mg/mL for E. coli DNA gyrase) but the lowest activity against HeLa cell topoisomerase II (IC50 = 265 mg/mL) among the quinolones tested.  Gatifloxacin is synergic with the beta-lactams piperacillin, cefepime and meropenem, and with gentamicin against some drug-resistant pathogens.  Gatifloxacin, an 8-methoxyfluoroquinolone, inhibits a staphylococcal efflux pump. Gatifloxacin combined with Ciprofloxacinplus shows synergy by the Etest method for 6 (19%) of the 31 P. aeruginosa isolates using a summation fractional inhibitory concentration of < or = 0.5 for synergy.  Gatifloxacin is two-fold less potent than ciprofloxacin, and the same as or two-fold more potent than ofloxacin against Enterobacteriaceae. Gatifloxacin is highly potent (MIC90s, 0.03-0.06 mg/L) against Haemophilus influenzae, Legionella spp., Helicobacter pylori and has at least eight-fold better anti-chlamydial and anti-mycoplasma potency (gatifloxacin MIC90s, 0.13 mg/L). 
|In vivo||Gatifloxacin decreases the serum glucose concentration in both normal and diabetic rats. Gatifloxacin results in an increase in the serum epinephrine concentration in both normal and diabetic rats. |
-  Alvirez-Freites EJ, et al. Antimicrob Agents Chemother, 2002, 46(4), 1022-1025.
-  Takei M, et al. Antimicrob Agents Chemother, 1998, 42(10), 2678-2681.
-  Dawis MA, et al. J Antimicrob Chemother, 2003, 51(5), 1203-1211.
|In vitro||DMSO||7 mg/mL (18.64 mM)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Synonyms||AM-1155, CG5501, BMS-206584|
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