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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).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $43 | In Stock | |
10 mg | $61 | In Stock | |
25 mg | $97 | In Stock | |
50 mg | $126 | In Stock | |
100 mg | $207 | In Stock | |
500 mg | $453 | In Stock | |
1 mL x 10 mM (in DMSO) | $53 | In Stock |
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). |
Targets&IC50 | GABA: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]. |
Alias | AH252723, A1443 |
Molecular Weight | 556.29 |
Formula | C22H17Cl2F6N3O3 |
Cas No. | 864731-61-3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 100 mg/mL (179.76 mM) H2O: Insoluble | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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