Idebenone，一种线粒体保护剂，具有神经保护功效，可用于研究阿尔茨海默病、亨廷顿舞蹈病，可透过血脑屏障。Idebenone (氧化形式) 对星形胶质细胞匀浆中花生四烯酸的酶代谢具有抑制作用 (IC50=16.65 μM)。 Idebenone 是一种辅酶 Q10 类似物和抗氧化剂，在人多巴胺能神经母细胞瘤 SHSY-5Y 细胞中诱导细胞凋亡 (apoptotic)。
| 生物活性 | Idebenone, a well-appreciated mitochondrial protectant, exhibits protective efficacy against neurotoxicity and can be used for the research of Alzheimer's disease, Huntington's disease. Idebenone (oxidised form) has a dose-dependent inhibitory effect on the enzymatic metabolism of arachidonic acid in astroglial homogenates (IC50=16.65 μM)[1]. Idebenone, a coenzyme Q10 analog and an antioxidant, inducesapoptoticcell death in the human dopaminergic neuroblastoma SHSY-5Y cells[2]. Idebenone quickly crosses the blood-brain barrier. |
体外研究
(In Vitro) | Idebenone, a compound with protective efficacy against neurotoxicity both in in vitro and in in vivo models, exists in two different oxidative states: the ubiquinol-derivative (reduced idebenone) and the ubiquinone-derivative (oxidised idebenone)[1].
Idebenone (oxidised form) preferentially inhibits cyclooxygenase vs. lipoxygenase metabolism (IC50ratio lipoxygenase/cyclooxygenase: 3.22)[1].
Idebenone (oxidised form) behaves similarly as indomethacin and piroxicam—two typical anti-inflammatory agents[1].
Idebenone (oxidised form) inhibits total arachidonic acid metabolism, cyclooxygenase metabolism, lipoxygenase metabolism, lipoxygenase/cyclooxygenase with IC50s of 16.65±3.48, 14.44±2.99, 46.51±7.20, and 3.22 μM[1].
Idebenone (1-10 μM; for 24-72 h) has no effect on the cell viability of SHSY-5Y cells[2].
Idebenone (25 μM or higher concentrations; for 24-72 h) shows significant reduction in cell viability of SHSY-5Y cells[2].
Idebenone (30 μM) induces up-regulation of BAX expression and the caspase-3 activity[2].
Cell Viability Assay[2] | Cell Line: | The human dopaminergic neuroblastma cell line, SHSY-5Y cells | | Concentration: | 1, 3, 10, 15, 25, 30, and 90 μM | | Incubation Time: | 24, 48, and 72 hours | | Result: | Had no apparent detrimental effects on cell viability as indicated by the absence of trypan blue-positive staining in the cells at concentrations of 1, 3, 10 μM.
Exhibited some degree of trypan blue-positive staining at 15 μM.
Showed extensive trypan blue-positive staining at 25 μM and 30 μM. |
RT-PCR[2] | Cell Line: | SHSY-5Y cells | | Concentration: | 10 μM, 30 μM | | Incubation Time: | 72 hours | | Result: | The total RNA of BAX from SHSY-5Y cells exposed to 10 μM was not different from that of the untreated control cells.
The BAX expression in SHSY-5Y cells exposed to 30 μM was significantly up-regulated when compared with the untreated control cells and cells exposed to 10 μM. |
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体内研究
(In Vivo) | Idebenone (oxidised form) is a compound with protective efficacy against cerebrovascular disorders in vivo, including cerebral ischemia and hypertension-induced vascular lesions[1].
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(295.47 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 2.9547 mL | 14.7737 mL | 29.5473 mL | | 5 mM | 0.5909 mL | 2.9547 mL | 5.9095 mL | | 10 mM | 0.2955 mL | 1.4774 mL | 2.9547 mL |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (7.39 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.39 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (7.39 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.39 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (7.39 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.39 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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