| Name | Fluralaner |
| Description | Fluralaner (A1443) is an isoxazoline ectoparasiticide. It potently and selectively inhibits binding of the GABA receptor channel blocker EBOB to housefly head membranes (IC50: 455 pM). |
| 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 [1]. 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) [2]. |
| 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 [2]. No adverse events were observed subsequent to fluralaner treatment of MDR1(-/-) Collies at three times the highest expected clinical dose [3]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (7.19 mM), Sonication is recommended.
DMSO : 250 mg/mL (449.41 mM), Sonication is recommended.
H2O : Insoluble
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| Keywords | Parasite | Inhibitor | inhibit | GABAReceptor | GABA Receptor | GABA | Fluralaner | AH-252723 | AH 252723 | A-1443 | A 1443 |
| Inhibitors Related | Gum arabic | Kojic acid | p-Hydroxybenzaldehyde | Urethane | Hydroxychloroquine | Metronidazole | Avermectin B1a | 2-Amino-2-methyl-1-propanol | Doxycycline | Penicillin G sodium salt | Fenpyroximate | Methylene Blue trihydrate |
| Related Compound Libraries | Anti-Parasitic Compound Library | Pain-Related Compound Library | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | EMA Approved Drug Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | Bioactive Compounds Library Max | Ion Channel Targeted Library | Anti-Cancer Drug Library |
United States
