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Fluralaner

Catalog No. T5330Cas No. 864731-61-3
Alias AH252723, A1443

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).

Fluralaner

Fluralaner

Purity: 99.90%
Catalog No. T5330Alias AH252723, A1443Cas No. 864731-61-3
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 SizePriceAvailabilityQuantity
5 mg$43In Stock
10 mg$61In Stock
25 mg$97In Stock
50 mg$126In Stock
100 mg$207In Stock
500 mg$453In Stock
1 mL x 10 mM (in DMSO)$53In Stock
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Purity:99.90%
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Product Introduction

Bioactivity
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].
AliasAH252723, A1443
Chemical Properties
Molecular Weight556.29
FormulaC22H17Cl2F6N3O3
Cas No.864731-61-3
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM1.7976 mL8.9881 mL17.9762 mL89.8812 mL
5 mM0.3595 mL1.7976 mL3.5952 mL17.9762 mL
10 mM0.1798 mL0.8988 mL1.7976 mL8.9881 mL
20 mM0.0899 mL0.4494 mL0.8988 mL4.4941 mL
50 mM0.0360 mL0.1798 mL0.3595 mL1.7976 mL
100 mM0.0180 mL0.0899 mL0.1798 mL0.8988 mL

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