Home DNA Damage/DNA Repair Topoisomerase inhibitor Gatifloxacin For research use only.

Gatifloxacin

Synonyms: AM-1155, CG5501, BMS-206584

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.

Gatifloxacin Chemical Structure

Gatifloxacin Chemical Structure

CAS: 112811-59-3

Selleck's Gatifloxacin has been cited by 2 Publications

1 Customer Review

Purity & Quality Control

Batch: S134001 DMSO] 7 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.62%
99.62

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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.
Targets
DNA gyrase [1] topoisomerase IV [1]
In vitro
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00905762 Completed Healthy Bausch & Lomb Incorporated March 2009 Phase 1
NCT00335231 Withdrawn Endophthalmitis Queen''s University June 2006 Not Applicable
NCT00382460 Completed Actue Coronary Syndromes Bristol-Myers Squibb November 2000 Phase 4

Chemical lnformation & Solubility

Molecular Weight 375.39 Formula

C19H22FN3O4
CAS No. 112811-59-3 SDF Download Gatifloxacin SDF
Smiles CC1CN(CCN1)C2=C(C=C3C(=C2OC)N(C=C(C3=O)C(=O)O)C4CC4)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 7 mg/mL ( (18.64 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

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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