product name Gatifloxacin
Description: Gatifloxacin (also known as AM-1155, CG5501, BMS-206584) is a fourth-generation antibiotic of the fluoroquinolone family, it inhibits the bacterial enzymes DNA gyrase and topoisomerase IV. 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. Gatifloxacin possesses potent inhibitory activities against bacterial type II topoisomerases but the lowest activity against HeLa cell topoisomerase II (IC50 = 265 mg/mL) among the quinolones tested.
References: Antimicrob Agents Chemother. 2002 Apr;46(4):1022-5; J Antimicrob Chemother. 2000 Apr;45(4):437-46.
375.39
Formula
C19H22FN3O4
CAS No.
112811-59-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 7 mg/mL (18.6 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
AM-1155, CG5501, BMS-206584
other peoduct :
| In Vitro |
In vitro activity: 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. 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. Gatifloxacin is synergic with the beta-lactams piperacillin, cefepime and meropenem, and with gentamicin against some drug-resistant pathogens. 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. 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). Kinase Assay: Cell Assay: |
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| 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. |
| Animal model | |
| Formulation & Dosage | |
| References | Antimicrob Agents Chemother. 2002 Apr;46(4):1022-5; J Antimicrob Chemother. 2000 Apr;45(4):437-46. |
