Fluralaner

SKU: orb1301882

Description

Fluralaner (A1443) is a potent isoxazoline-class ectoparasiticide that acts by selectively inhibiting insect GABA-gated chloride channels, demonstrated by its high-affinity displacement of EBOB in housefly head membrane assays (IC50 = 455 pM). It is widely used in veterinary parasitology research for studying ectoparasite control and has applications in both in vitro receptor binding studies and in vivo efficacy models against ticks and fleas.

Research Area

Infectious Disease & Virology, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 864731-61-3
• MW: 556.285
• Purity: 99.72% (May vary between batches)
• Formula: C₂₂H₁₇Cl₂F₆N₃O₃
• SMILES: O=C(NCC(NCC(F)(F)F)=O)C1=CC=C(C2=NOC(C(F)(F)F)(C3=CC(Cl)=CC(Cl)=C3)C2)C=C1C
• Target: GABA Receptor,Parasite
• Solubility: H2O:Insoluble;10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (7.19 mM);DMSO:100 mg/mL (179.76 mM)

Bioactivity

• Target IC50:
  GABA:455 pM
• In Vivo:
  In the simulated flea-infested home environment, flea-control efficacy on fluralaner-treated dogs was >99% at every time point measured for 12 weeks. No adverse events were observed in fluralaner-treated dogs . No adverse events were observed subsequent to fluralaner treatment of MDR1(-/-) Collies at three times the highest expected clinical dose .
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• In Vitro:
  A1443 inhibits specific binding of the gamma-aminobutyric acid (GABA) receptor channel blocker EBOB to housefly-head membranes, with an IC(50) value of 455pM. In contrast, the IC(50) value in rat-brain membranes is>10muM. A1443 blocks GABA- and glutamate-induced chloride currents in Xenopus oocytes expressing MdGBCl or MdGluCl channels, with IC(50) values of 5.32 and 79.9 nM, respectively . Fluralaner potently inhibited flea reproduction capacity in vitro. Oviposition ceased completely at concentrations as low as 25.0 ng/mL. While no ovicidal effect was observed, fluralaner exerted a larvicidal effect at exceptionally low concentrations (6.25 ng/mL) .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Parasite, inhibit, Fluralaner, GABAReceptor, GABA Receptor, GABA, Inhibitor, AH252723, AH-252723, AH 252723, A1443, A-1443, A 1443

Compound Identifiers

PubChem CID

25144319