Fluxametamide

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Fluxametamide 是一种新型异恶唑啉杀虫剂，通过对昆虫配体门控氯通道的独特拮抗作用发挥作用，作为 GABA 和谷氨酸门控氯通道的拮抗剂。

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 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. 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 shows significant insecticidal activity with an LD50 (LD95) value of 12.9 ± 4.9 ng/fly (38.7 ± 6.3 ng/fly).

——

Membrane Transporter/Ion Channel

Other Targets

GABA

——

——

928783-29-3

474.26

C20H16Cl2F3N3O3

>98% (HPLC)

DMSO:125 mg/mL (263.57 mM; Need ultrasonic);H2O:< 0.1 mg/mL (insoluble)

CC1=C(C=CC(=C1)C2=NOC(C2)(C3=CC(=CC(=C3)Cl)Cl)C(F)(F)F)C(=O)N/C=N/OC

——

(-20℃)

With Ice Pack

≥ 2 years