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Fluralaner

Catalog No. T5330 CAS 864731-61-3

Synonyms: 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).

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Fluralaner, CAS 864731-61-3

Pack Size	Availability	Price/USD
5 mg	In stock	$ 43.00
10 mg	In stock	$ 61.00
25 mg	In stock	$ 97.00
50 mg	In stock	$ 126.00
100 mg	In stock	$ 207.00
500 mg	In stock	$ 453.00
1 mL * 10 mM (in DMSO)	In stock	$ 53.00

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Purity: 99.90%

Purity: 99.77%

Purity: 99.72%

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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].

Synonyms	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

Solubility Information

DMSO: 100 mg/mL (179.76 mM)

H2O: Insoluble

References and Literature

1. Ozoe Y, et al. The antiparasitic isoxazoline A1443 is a potent blocker of insect ligand-gated chloride channels. Biochem Biophys Res Commun. 2010 Jan 1;391(1):744-9. 2. Williams H, et al. Fluralaner, a novel isoxazoline, prevents flea (Ctenocephalides felis) reproduction in vitro and in asimulated home environment. Parasit Vectors. 2014 Jun 19;7:275. 3. Wang K, Li B, Yu Y, et al. Bacterial Rdl2 dsRNA increased the insecticidal activity of GABAR blockers and allosteric modulators against Plutella xylostella[J]. bioRxiv. 2021 4. Zahran F, El-Din H M E, Shehata M A S. Study on the effect of an ion channel inhibitor “Fluralaner” on Echinococcus granulosus protoscolices and metacestode layers in vitro[J]. Journal of Parasitic Diseases. 2020, 44(2): 411-419. 5. Zahran F, El-Din H M E, Shehata M A S. Study on the effect of an ion channel inhibitor ‘‘Fluralaner’’on Echinococcus granulosus protoscolices and metacestode layers in vitro[J]. Journal of Parasitic Diseases: Official Organ of the Indian Society for Parasitology. 2020, 44(2): 411-419.

Citations

1. Gastaldi M S, Felsztyna I, Miguel V, et al.Theoretical and Experimental Study of Molecular Interactions of Fluralaner with Lipid Membranes.Journal of Agricultural and Food Chemistry.2023 2. Li B J, Wang K K, Yu Y, et al.PxRdl2 dsRNA increased the insecticidal activities of GABAR-targeting compounds against Plutella xylostella.Pesticide Biochemistry and Physiology.2023: 105548.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Drug Repurposing Compound Library Anti-Parasitic Compound Library Anti-Cancer Approved Drug Library Inhibitor Library Anti-Neurodegenerative Disease Compound Library NO PAINS Compound Library Ion Channel Inhibitor Library Bioactive Compound Library Anti-Cancer Compound Library

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Keywords

Fluralaner 864731-61-3 Membrane transporter/Ion channel Microbiology/Virology Neuroscience GABA Receptor Parasite A-1443 AH252723 inhibit AH-252723 A1443 A 1443 AH 252723 Inhibitor inhibitor

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