Fleroxacin

Fleroxacin, a quinolone, is a bactericidal drug that inhibits bacterial DNA gyrase and topoisomerase IV. Like other quinolones and fluoroquinolones the compound eradicates bacteria by interfering with DNA replication (bacterial DNA replication, transcription, repair and recombination). Fleroxacin is active against many Gram-positive and Gram-negative bacteria.

Product information

CAS Number: 79660-72-3

Molecular Weight: 369.34

Formula: C17H18F3N3O3

Synonym:

Quinodis

Megalocin

AM-833

Megalone

AM833

AM 833

Chemical Name: 6,8-difluoro-1-(2-fluoroethyl)-7-(4-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid

Smiles: CN1CCN(CC1)C1=C(F)C2=C(C=C1F)C(=O)C(=CN2CCF)C(O)=O

InChiKey: XBJBPGROQZJDOJ-UHFFFAOYSA-N

InChi: InChI=1S/C17H18F3N3O3/c1-21-4-6-22(7-5-21)15-12(19)8-10-14(13(15)20)23(3-2-18)9-11(16(10)24)17(25)26/h8-9H,2-7H2,1H3,(H,25,26)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: 0.1 M NaOH : 9.17 mg/mL (24.83 mM; ultrasonic and adjust pH to 12 with NaOH)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vivo:

Fleroxacin (Ro 23-6240) is a new trifluorinated quinolone exhibiting high activity against a broad spectrum of gram-negative and gram-positive bacteria. Fleroxacin is characterized pharmacokinetically by a long elimination half-life (9 to 10 h) and high concentrations in plasma (e.g., maximum concentration of 2.3 micrograms/ml after an oral dose of 200 mg). Fleroxacin (Ro 23-6240) is effective against Haemophilus ducreyi in vitro. Fleroxacin (Ro 23-6240), 200 or 400 mg as a single oral dose, is efficacious therapy for microbiologically proven chancroid in patients who do not have concurrent HIV-1 infection. Among HIV-1-infected men, a single dose of 200 or 400 mg of fleroxacin is inadequate therapy for chancroid.

References:

1. Weidekamm, E., et al., Single- and multiple-dose pharmacokinetics of fleroxacin, a trifluorinated quinolone, in humans. Antimicrob Agents Chemother, 1987. 31(12): p. 1909-14.
2. MacDonald, K.S., et al., Evaluation of fleroxacin (RO 23-6240) as single-oral-dose therapy of culture-proven chancroid in Nairobi, Kenya. Antimicrob Agents Chemother, 1989. 33(5): p. 612-4.

Products are for research use only. Not for human use.