Gatifloxacin

SKU: orb1309089

Description

Gatifloxacin (CG5501) is a fourth-generation fluoroquinolone antibiotic that inhibits bacterial DNA gyrase and topoisomerase IV. It is widely used in research for studying antibacterial mechanisms and efficacy in both in vitro susceptibility assays and in vivo infection models.

Research Area

Infectious Disease & Virology, Molecular Biology, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 112811-59-3
• MW: 375.39
• Purity: 99.96% (May vary between batches)
• Formula: C₁₉H₂₂FN₃O₄
• SMILES: O(C)C1=C2N(C=C(C(O)=O)C(=O)C2=CC(F)=C1N3CC(C)NCC3)C4CC4
• Target: Antibiotic|||Topoisomerase|||Antibacterial
• Solubility: DMSO:3.8 mg/mL (10.12 mM)

Bioactivity

• Target IC50:
  Topo II:36.7 μM (IC50)
• In Vivo:
  Gatifloxacin exhibits potent inhibitory activity against bacterial type II topoisomerases, with half-maximal inhibitory concentrations (IC50) of 13.8 mg/mL and 0.109 mg/mL for Staphylococcus aureus topoisomerase and Escherichia coli DNA gyrase, respectively. Its inhibitory effect on HeLa cell topoisomerase II is minimal, with an IC50 of 265 mg/mL. Gatifloxacin inhibits Mycobacterium tuberculosis ATCC 35801 with a minimum inhibitory concentration (MIC) of 0.125 μg/mL. When used in combination with ciprofloxacin, gatifloxacin demonstrates a synergistic effect on 19% of 31 strains of Pseudomonas aeruginosa. However, gatifloxacin's activity is two-fold lower than that of ciprofloxacin and two-fold less potent than ofloxacin against Enterobacteriaceae. Gatifloxacin shows strong antimicrobial activity against Haemophilus influenzae, Legionella, and Helicobacter pylori (MIC90s, 0.03-0.06 mg/L), and at least an eight-fold greater efficacy against Chlamydiaceae and Mycoplasmataceae (gatifloxacin MIC90s, 0.13 mg/L).
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• In Vitro:
  Gatifloxacin increases serum adrenaline levels in both normal and diabetic rats, and concurrently reduces serum glucose concentrations in these subjects.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Topoisomerase, Topo IV, hypoglycemia, N. brasiliensis, PD 135432, PD135432, PD-135432, E. coli,?Pseudomonas aeruginosa,?Micrococcus luteus, conjunctivitis, CG5501, CG-5501, CG 5501, Antibiotic, Bacterial, BMS 206584, BMS 206584-01, BMS206584, BMS-206584, actinomycetoma, AM1155, AM-1155, AM 1155

Compound Identifiers

PubChem CID

5379