Gatifloxacin

Catalog No.S1340 Synonyms: AM-1155, CG5501, BMS-206584

Gatifloxacin Chemical Structure

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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In DMSO USD 130 In stock
USD 97 In stock
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Cited by 1 Publication

1 Customer Review

  • 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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Biological Activity

Description Gatifloxacin is an antibiotic of the fourth-generation fluoroquinolone family, and inhibits the bacterial enzymes DNA gyrase and topoisomerase IV.
Targets
DNA gyrase [1] topoisomerase IV [1]
In vitro

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. [1] 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. [2] Gatifloxacin is synergic with the beta-lactams piperacillin, cefepime and meropenem, and with gentamicin against some drug-resistant pathogens. [3] 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. [4] 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). [5]

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. [6]

Protocol

Solubility (25°C)

In vitro DMSO 7 mg/mL (18.64 mM)
Water Insoluble
Ethanol Insoluble

* 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.

Chemical Information

Molecular Weight 375.39
Formula

C19H22FN3O4

CAS No. 112811-59-3
Storage powder
in solvent
Synonyms AM-1155, CG5501, BMS-206584

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03578276 Recruiting Cataract Carolina Eyecare Physicians LLC|Science in Vision|Imprimis Pharmaceuticals Inc. June 22 2018 Phase 4
NCT03578276 Recruiting Cataract Carolina Eyecare Physicians LLC|Science in Vision|Imprimis Pharmaceuticals Inc. June 22 2018 Phase 4
NCT02717871 Unknown status Keratitis; Infectious Disease (Manifestation) University Hospital Geneva March 2016 Phase 3
NCT02717871 Unknown status Keratitis; Infectious Disease (Manifestation) University Hospital Geneva March 2016 Phase 3
NCT02196740 Unknown status Periapical Diseases Lin Jiacheng|Sun Yat-sen University June 2013 Not Applicable
NCT02196740 Unknown status Periapical Diseases Lin Jiacheng|Sun Yat-sen University June 2013 Not Applicable

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Topoisomerase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID