Flumequine

SKU: orb1309907

Description

Flumequine

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 42835-25-6
• MW: 261.25
• Purity: 99.40% (May vary between batches)
• Formula: C₁₄H₁₂FNO₃
• SMILES: O=C1C=2C=3N(C=C1C(O)=O)C(C)CCC3C=C(F)C2
• Target: Topoisomerase,Antibacterial,Antibiotic
• Solubility: Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:3 mg/mL (11.48 mM)

Bioactivity

• Target IC50:
  Topo II:15 μM
• 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.
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Antibiotic, Bacterial, inhibit, Flumigal, Flumequine, Inhibitor, Topo II, Topoisomerase, R 802, R802, R-802

Compound Identifiers

PubChem CID

3374