Rotenone是一种线粒体电子传递链复合物 I 的抑制剂，IC50值范围为1.7至2.2 μM。它通过促进线粒体活性氧的生成诱导细胞凋亡，并抑制 NADH/DB氧化还原酶的活性。
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HazMat fee for 500 gram (Estimated)
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Limited Quantity
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Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
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Accessible (Haz class 3, 4, 5 or 8), International
Rotenone is a classical mitochondrial complex I inhibitor that blocks the electron transfer of mitochondrial respiration chain. It inhibits NADH oxidase and NADH/DB oxidoreductase with IC50 values of 5.1 and 28.8 nM, respectively[1]. Rotenone blocked the proliferation of MCF-7 and Hela cells by inhibiting the reassembly of microtubules with half inhibitory concentrations of 0.4 and 0.2 μM, respectively[2]. In substantia nigra pars compacta neurons, 1 μM rotenone stimulated a tolbutamide-sensitive outward current (94 pA) accompanied with the accumulation of intracellular [Na+] and [Ca2+] [3]. Rotenone infusion (2 mg/kg/day for 2 days) in Lewis rats resulted in reduced binding of [3H]dihydrorotenone and complex I throughout the brain, while the enzymatic activities of cytochrome oxidase and succinate dehydrogenase remained unaffected. Systemic rotenone infusion (2.5 mg/kg/day) for 7 – 33 days led to progressive nigrostriatal dopaminergic degeneration in the brain. Compared to nigral cell bodies, striatal nerve terminals were affected more severely and earlier by rotenone infusion[4].
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