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Antofloxacin

Catalog No. T38581   CAS 119354-43-7

Antofloxacin is a well-tolerated, orally active, and broad-spectrum 8-amino-fluoroquinolone compound that exhibits potent antibacterial properties. It demonstrates superior activity against gyrA mutation-positive Helicobacter pylori strains, particularly in strains with mutations in the Asn87 position, when compared to levofloxacin. Additionally, Antofloxacin acts as a weak but reversible inhibitor of CYP1A2 and is clinically used to treat infections caused by various bacterial species.

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Antofloxacin Chemical Structure
Antofloxacin, CAS 119354-43-7
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Antofloxacin is a well-tolerated, orally active, and broad-spectrum 8-amino-fluoroquinolone compound that exhibits potent antibacterial properties. It demonstrates superior activity against gyrA mutation-positive Helicobacter pylori strains, particularly in strains with mutations in the Asn87 position, when compared to levofloxacin. Additionally, Antofloxacin acts as a weak but reversible inhibitor of CYP1A2 and is clinically used to treat infections caused by various bacterial species.
In vivo Administered subcutaneously to mice at doses ranging from 2.5 to 160 mg/kg over a 24-hour period, antofloxacin's penetration ratio for total drug concentrations varied between 1.22 and 1.54, showing no relation to the dosage levels [3]. Additionally, antofloxacin elevates plasma theophylline levels by functioning as a mechanism-based inhibitor of the CYP1A2 enzyme. This inhibition effect on the formation of the three metabolites of theophylline demonstrates a dependency on time, concentration, and the presence of NADPH, indicative of mechanism-based inhibition [2].
Molecular Weight 376.388
Formula C18H21FN4O4
CAS No. 119354-43-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. He XJ, et al. Efficacy and Safety of Antofloxacin-Based Triple Therapy for Helicobacter pylori Eradication Failure in China [published online ahead of print, 2021 Feb 8]. Dig Dis Sci. 2021;10.1007/s10620-021-06856-z. 2. Liu L, et al. Modulation of pharmacokinetics of theophylline by antofloxacin, a novel 8-amino-fluoroquinolone, in humans. Acta Pharmacol Sin. 2011;32(10):1285-1293. 3. Zhou YF, et al. In Vivo Pharmacokinetic and Pharmacodynamic Profiles of Antofloxacin against Klebsiella pneumoniae in a Neutropenic Murine Lung Infection Model. Antimicrob Agents Chemother. 2017;61(5):e02691-16. Published 2017 Apr 24.

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Antofloxacin 119354-43-7 inhibitor inhibit

 

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