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

2 publications

Gatifloxacin Chemical Structure

CAS No. 112811-59-3

Gatifloxacin (AM-1155, CG5501, BMS-206584) is an antibiotic of the fourth-generation fluoroquinolone family, and inhibits the bacterial enzymes DNA gyrase and topoisomerase IV.

Selleck's Gatifloxacin has been cited by 2 publications

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 (AM-1155, CG5501, BMS-206584) is an antibiotic of the fourth-generation fluoroquinolone family, and inhibits the bacterial enzymes DNA gyrase and topoisomerase IV.
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]


Solubility (25°C)

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

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Chemical Information

Molecular Weight 375.39


CAS No. 112811-59-3
Storage powder
in solvent
Synonyms AM-1155, CG5501, BMS-206584
Smiles CC1CN(CCN1)C2=C(C=C3C(=C2OC)N(C=C(C3=O)C(=O)O)C4CC4)F

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00905762 Completed Drug: Gatifloxacin|Drug: Moxifloxacin|Drug: Besifloxacin Healthy Bausch & Lomb Incorporated March 2009 Phase 1
NCT00335231 Withdrawn Drug: gatifloxacin ophthalmic (ZYMAR) Endophthalmitis Queen''s University June 2006 Not Applicable
NCT00382460 Completed Drug: PRAVASTATIN SODIUM Actue Coronary Syndromes Bristol-Myers Squibb November 2000 Phase 4

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Topoisomerase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID