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Gatifloxacin Topoisomerase inhibitor

Cat.No.S1340

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 Topoisomerase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 375.39

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 7 mg/mL (18.64 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous 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.

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Chemical Information, Storage & Stability

Molecular Weight 375.39 Formula

C19H22FN3O4

 Storage (From the date of receipt)
CAS No. 112811-59-3 Download SDF Storage of Stock Solutions

Synonyms AM-1155, CG5501, BMS-206584 Smiles CC1CN(CCN1)C2=C(C=C3C(=C2OC)N(C=C(C3=O)C(=O)O)C4CC4)F

Mechanism of Action

Targets/IC50/Ki
DNA gyrase
topoisomerase IV
In vitro
Gatifloxacin has somewhat better in vitro activity against M. tuberculosis than moxifloxacin, and both are much more active than levofloxacin. This compound is against M. tuberculosis ATCC 35801 with MICs of 0.125 μg/mL. It 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. This agent is synergic with the beta-lactams piperacillin, cefepime and meropenem, and with gentamicin against some drug-resistant pathogens. It inhibits a staphylococcal efflux pump. This chemical 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. It is two-fold less potent than ciprofloxacin, and the same as or two-fold more potent than ofloxacin against Enterobacteriaceae. It 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. This compound results in an increase in the serum epinephrine concentration in both normal and diabetic rats.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/15980375/
  • [5] https://pubmed.ncbi.nlm.nih.gov/10747819/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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