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Fluxametamide

Catalog No. T11307 CAS 928783-29-3

Fluxametamide is a novel isoxazoline insecticide that acts via distinctive antagonism of insect ligand-gated chloride channels, acts as an antagonist of GABA- and glutamate-gated chloride channels(IC50 of 1.95 nM and 225 nM for M. domestica GABACls and GluCls).

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Fluxametamide, CAS 928783-29-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 41.00
5 mg	In stock	$ 97.00
10 mg	In stock	$ 155.00
25 mg	In stock	$ 293.00
50 mg	In stock	$ 538.00
100 mg	In stock	$ 768.00
1 mL * 10 mM (in DMSO)	In stock	$ 98.00

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Purity: 99.83%

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Description	Fluxametamide is a novel isoxazoline insecticide that acts via distinctive antagonism of insect ligand-gated chloride channels, acts as an antagonist of GABA- and glutamate-gated chloride channels(IC50 of 1.95 nM and 225 nM for M. domestica GABACls and GluCls).
Targets&IC50	GABACls (M. domestica):1.95 nM , GluCls (M. domestica):225 nM
In vitro	Fluxametamide inhibits GABA responses in the wild-type L. striatellus GABACls with IC50 values of 1.40 (0.57-3.29) nM; in the A2′N mutant GABACls, the IC50 value is 3.51 (2.17-5.69) nM. Moreover, Fluxametamide scarcely inhibits GABA (EC50)-induced currents in rat GABACls at 10 μM and with no inhibition on glycine (EC50)-induced current in human α1 GlyCls at tested concentrations.Fluxametamide is an antagonist of GABA- and glutamate-gated chloride channels, dose-dependently inhibits currents induced by GABA and glutamate in M. domestica GABACls and GluCls, with IC50 values of 1.95 (1.18-3.21) nM and 225 (137-372) nM, respectively, and displays potent antagonistic activity against T. urticae GABACls with an IC50 of 0.219 (0.127-0.381) nM.
In vivo	Fluxametamide exerts distinctive antagonism of arthropod GABACls by binding to a site different from those for existing antagonists.In contrast to its profound actions on the arthropod LGCCs, the antagonistic activity of fluxametamide against rat GABACls and human glycine-gated chloride channels was nearly insignificant, suggesting that fluxametamide has high target-site selectivity for arthropods over mammals.Overall, fluxametamide is a new type of LGCC antagonist insecticide with excellent safety for mammals at the target-site level.

Molecular Weight	474.26
Formula	C20H16Cl2F3N3O3
CAS No.	928783-29-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 125 mg/mL (263.57 mM), Sonification is recommended.

References and Literature

1. MihoAsahi, et al. Fluxametamide: A novel isoxazoline insecticide that acts via distinctive antagonism of insect ligand-gated chloride channels. Pesticide Biochemistry and Physiology. 2. 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

Citations

1. 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-Neurodegenerative Disease Compound Library Inhibitor Library Neuronal Signaling Compound Library Ion Channel Inhibitor Library Bioactive Compound Library Anti-Cancer Compound Library Anti-Parkinson's Disease Compound Library NO PAINS Compound Library Bioactive Compounds Library Max Neurotransmitter Receptor Compound Library

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Keywords

Fluxametamide 928783-29-3 Membrane transporter/Ion channel Neuroscience GABA Receptor inhibit Inhibitor γ-Aminobutyric acid Receptor Gamma-aminobutyric acid Receptor inhibitor

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