Fluxametamide 是一种广谱杀虫剂和 GABA 及谷氨酸门控氯离子通道拮抗剂,其对 M. domestica 中的 GABACl 和 GluCl 的 IC50 值分别为 1.95 nM 和 225 nM。
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描述 | Fluxametamide is a new type of LGCC (ligand-gated chloride channel) antagonist insecticide with excellent safety for mammals at the target-site level. Fluxametamide potently inhibited the specific binding of [3H]EBOB to housefly-head membranes, suggesting that fluxametamide affects insect γ-aminobutyric acid (GABA)-gated chloride channels (GABACls). Next, the antagonism of housefly GABACls and glutamate-gated chloride channels (GluCls) was examined using the two-electrode voltage clamp (TEVC) method. Fluxametamide inhibited agonist responses in both ion channels expressed in Xenopus oocytes in the nanomolar range, indicating that this insecticide is a ligand-gated chloride channel (LGCC) antagonist. 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[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.11mL 0.42mL 0.21mL |
10.54mL 2.11mL 1.05mL |
21.09mL 4.22mL 2.11mL |
CAS号 | 928783-29-3 |
分子式 | C20H16Cl2F3N3O3 |
分子量 | 474.261 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Sealed in dry,2-8°C |
溶解度 |
DMSO: 120 mg/mL(253.03 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |