|4-[5-(3,5-二氯苯基)-4,5-二氢-5-(三氟甲基)-3- 异恶唑基]-N-[(甲氧基胺基)亚甲基]-2-甲基苯甲酰胺|CsnPharm

CAS No.: 928783-29-3

Fluxametamide/氟甲酰胺 Catalog No. CSN22401

Synonyms: Fluxametamide

Fluxametamide is an insecticide with wide spectrum, acts as an antagonist of GABA- and glutamate-gated chloride channels, with IC50 of 1.95  nM and 225  nM for M. domestica GABACls and GluCls.

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400-920-2911

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技术信息

生物活性

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].
参考文献

[1] Asahi M, Kobayashi M, Kagami T, Nakahira K, Furukawa Y, Ozoe Y. Fluxametamide: A novel isoxazoline insecticide that acts via distinctive antagonism of insect ligand-gated chloride channels. Pestic Biochem Physiol. 2018 Oct;151:67-72

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1085 mL
- 10.5427 mL
- 21.0855 mL
- 5 mM
- 0.4217 mL
- 2.1085 mL
- 4.2171 mL
- 10 mM
- 0.2109 mL
- 1.0543 mL
- 2.1085 mL

技术信息

CAS号

928783-29-3

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H16Cl2F3N3O3

运输

蓝冰

分子量

474.26

别名

Fluxametamide

溶解度

DMSO	120.0 mg/mL (253.0 mM) warming
Water	Insoluble

动物实验配方

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Fluxametamide/氟甲酰胺 Catalog No. CSN22401

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