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Flumequine

Catalog No. T1060 CAS 42835-25-6

Synonyms: Flumigal, R-802

Flumequine (R-802) is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria. It functions by inhibiting DNA gyrase, a type II topoisomerase, and topoisomerase IV, enzymes necessary to separate bacterial DNA, thereby inhibiting cell division.

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Flumequine, CAS 42835-25-6

Pack Size	Availability	Price/USD
50 mg	In stock	$ 33.00
100 mg	In stock	$ 46.00
200 mg	In stock	$ 63.00
1 mL * 10 mM (in DMSO)	In stock	$ 51.00

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Purity: 99.4%

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Description	Flumequine (R-802) is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria. It functions by inhibiting DNA gyrase, a type II topoisomerase, and topoisomerase IV, enzymes necessary to separate bacterial DNA, thereby inhibiting cell division.
Targets&IC50	Topo II:15 μM
In vitro	At a concentration of 100 mg/L, Flumequine reduced the average length of roots, hypocotyls, and cotyledons in the water plant Lythrum salicaria L., and diminished the count of secondary roots. After oral administration of 10 mg/kg Flumequine, the total clearance rates were 0.024 L/h.kg (cod) and 0.14 L/h.kg (dab), with elimination half-lives (t1/2 λ z) of 75 hours (cod) and 31 hours (dab). The bioavailability of Flumequine following oral administration was measured at 65% (cod) and 41% (dab). Dose-dependent DNA damage in the stomach, colon, and bladder of adult mice was observed after oral administration of 4000 ppm Flumequine for 3 hours instead of 24 hours. In Atlantic salmon, the stable apparent volume of distribution was 3.5 L/kg after intravenous administration of Flumequine, with an elimination half-life (t 1/2) of 22.8 hours, and the area under the plasma drug concentration-time curve (AUC) was 140 µg×hour/mL.
In vivo	Flumequine demonstrates a minimum inhibitory concentration (MIC) ranging from 0.06 μg/mL to 32 μg/mL across 12 clinically isolated Salmonella strains. The high E(max) values for most resistant strains, reaching up to 16, indicate its significant contribution to combating resistant phenotypes. Accumulation studies have shown that these high E(max) values correlate with lower levels of accumulation. Flumequine's inhibition of eukaryotic topoisomerase II, associated with the double-stranded DNA breakage reaction, is the underlying cause for its effect on bacterial gyrase, suggesting a strong correlation between its action on topoisomerase II and the bacterial gyrase inhibition.

Synonyms	Flumigal, R-802
Molecular Weight	261.25
Formula	C14H12FNO3
CAS No.	42835-25-6

Storage

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

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 3 mg/mL (11.48 mM)

References and Literature

1. Kashida Y, et al. Toxicol Sci, 2002, 69(2), 317-321. 2. Giraud E, et al. J Med Microbiol, 2004, 53(Pt 9), 895-901. 3. Martinsen B, et al. Antimicrob Agents Chemother, 1995, 39(5), 1059-1064. 4. Migliore L, et al. Chemosphere, 2000, 40(7), 741-750. 5. Hansen MK, et al. J Vet Pharmacol Ther, 2000, 23(3), 163-168. 6. Aller-Morán LM, et al. Evaluation of the in vitro activity of flumequine against field isolates of Brachyspira hyodysenteriae. Res Vet Sci. 2015 Dec;103:51-3.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Fluorochemical Library Bioactive Compounds Library Max Human Metabolite Library Antibiotics Library NO PAINS Compound Library FDA-Approved & Pharmacopeia Drug Library Immunology/Inflammation Compound Library Orally Active Compound Library Bioactive Compound Library

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Keywords

Flumequine 42835-25-6 DNA Damage/DNA Repair Microbiology/Virology Topoisomerase Antibacterial Antibiotic Flumigal inhibit Inhibitor Bacterial R802 R 802 R-802 inhibitor

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