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Fluxametamide

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Catalog No. T11307Cas No. 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).

Fluxametamide

Fluxametamide

🥰Excellent
Purity: 99.83%
Catalog No. T11307Cas No. 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).
Pack SizePriceAvailabilityQuantity
1 mg$32In Stock
5 mg$73In Stock
10 mg$123In Stock
25 mg$263In Stock
50 mg$428In Stock
100 mg$662In Stock
1 mL x 10 mM (in DMSO)$80In Stock
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Purity:99.83%
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Product Introduction

Bioactivity
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 Gl
Targets&IC50
GluCls (M. domestica):225 nM , GABACls (M. domestica):1.95 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.
Chemical Properties
Molecular Weight474.26
FormulaC20H16Cl2F3N3O3
Cas No.928783-29-3
SmilesCON\C=N\C(=O)c1ccc(cc1C)C1=NOC(C1)(c1cc(Cl)cc(Cl)c1)C(F)(F)F
Relative Density.1.43 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 125 mg/mL (263.57 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.1085 mL10.5427 mL21.0855 mL105.4274 mL
5 mM0.4217 mL2.1085 mL4.2171 mL21.0855 mL
10 mM0.2109 mL1.0543 mL2.1085 mL10.5427 mL
20 mM0.1054 mL0.5271 mL1.0543 mL5.2714 mL
50 mM0.0422 mL0.2109 mL0.4217 mL2.1085 mL
100 mM0.0211 mL0.1054 mL0.2109 mL1.0543 mL

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