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：

Pure form Keep in dark place,Inert atmosphere,Room temperature

In solvent -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].
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.

[6]Liu J, Liu W, Lu Y, Tian H, Duan C, Lu L, Gao G, Wu X, Wang X, Yang H. Piperlongumine restores the balance of autophagy and apoptosis by increasing BCL2 phosphorylation in rotenone-induced Parkinson disease models. Autophagy. 2018;14(5):845-861.