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编 号:F068008
分子式:C12H4Cl2F6N4OS
分子量:437.15
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10mM*1mL in DMSO
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25mg
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50mg
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100mg
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生物活性:
Fipronil is a broad-spectrum insecticide effective against Lepidoptera species as well as thrips, locusts, ants, cockroaches, fleas and ticks. Fipronil selectively inhibits GABA receptor with IC50s of 30 nM and 1600 nM for cockroach and rat GABA receptors, respectively. Glutamate-gated chloride channels (GluCls), which are present in cockroaches but not in mammals, are sensitive to the blocking effect of Fipronil. Fipronil also induces apoptosis in HepG2 cells and promotes the expression of CYP1A1 and CYP3A4 mRNA in human hepatocytes.

体内研究:
氟虫腈抑制两种谷氨酸诱导的氯离子脱敏和非脱敏电流,IC50 值分别为 800 和 10 nM。氟虫腈对蟑螂 GABA 受体的选择性比对大鼠 GABA 的选择性更大。氟虫腈在静止和激活状态下都能阻断蟑螂的 GABA 受体,其 IC50 值分别为 28 和 35 nM。

体外研究:
氟虫腈 (0.1-25 μM; 72 h) 剂量依赖性地诱导人类肝细胞中 CYP1A1 和 CYP3A4 mRNA 的表达。氟虫腈 (0.1-25 μM; 72 h) 以时间和剂量依赖的方式诱导 HepG2 细胞中的 caspase-3/7 (caspase-3/7活性是细胞凋亡过程的重要标志物)。
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