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Rotenone

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Chemical Structure| 83-79-4 同义名 : Nicouline;Barbasco;Ro-KO;HSDB 1762;Ronone;bCube-Pulver;Cube root;Tubatoxin;NSC 26258;NSC 8505;Rotocide;Rotenon;Paraderil;Dactinol
CAS号 : 83-79-4
货号 : A360385
分子式 : C23H22O6
纯度 : 99%
分子量 : 394.417
MDL号 : MFCD09025614
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(126.77 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：
生物活性
描述 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].
作用机制 Rotenone is a lipophilic inhibitor for complex I in mitochondrial electron transport chain that blocks the electron transfer from complex I to ubiquinone, thereby inhibiting oxidative phosphorylation and suppressing the synthesis of ATP[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.54mL

0.51mL

0.25mL

12.68mL

2.54mL

1.27mL

25.35mL

5.07mL

2.54mL
参考文献

[1]Tormo JR, Gallardo T, et al. Inhibitory effects on mitochondrial complex I of semisynthetic mono-tetrahydrofuran acetogenin derivatives. Bioorg Med Chem Lett. 2003;13(22):4101-5.

[2]Srivastava P, Panda D. Rotenone inhibits mammalian cell proliferation by inhibiting microtubule assembly through tubulin binding. FEBS J. 2007;274(18):4788-801.

[3]Freestone PS, Chung KK, et al. Acute action of rotenone on nigral dopaminergic neurons--involvement of reactive oxygen species and disruption of Ca2+ homeostasis. Eur J Neurosci. 2009;30(10):1849-59.

[4]Betarbet R, Sherer TB, et al. Chronic systemic pesticide exposure reproduces features of Parkinson's disease. Nat Neurosci. 2000;3(12):1301-6.

[5]Heinz S, Freyberger A, et al. Mechanistic Investigations of the Mitochondrial Complex I Inhibitor Rotenone in the Context of Pharmacological and Safety Evaluation. Sci Rep. 2017.