Dihydrorotenone是一种杀虫剂，是线粒体复合物I的不可逆抑制剂，并且能够穿过血脑屏障。
Cas No.:6659-45-6
Sample solution is provided at 25 µL, 10mM.
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Dihydrorotenone is an insecticide and irreversible inhibitor of mitochondrial complex I and can cross the blood-brain barrier [1]. Dihydrorotenone binds to and inhibits the complex I in the electron transport chain, thus inhibiting mitochondrial function and decreasing ATP production[2]. Dihydrorotenone can be labeled for use in radioautography to investigate the unique distribution of complex I in the brain[3].
In vitro, Dihydrorotenone treatment at 20µM for 24 hours triggered endoplasmic reticulum stress and activated the p38 signaling pathway, leading to apoptosis of KMS11 cells[4]. Treatment with 15µM Dihydrorotenone for 24 hours inhibited the expression of cell cycle proteins, causing LP1 cells to be arrested in the G0/G1 phase and reducing the phosphorylation levels of AKT and ERK[5]. After 2 weeks of treatment with 1µM Dihydrorotenone, the expressions of FSP1, PDGFRα and PDGFRβ in SCAF#36 cells significantly decreased, the expression of pro-inflammatory cytokine genes was significantly downregulated, and the cell viability significantly declined[6].
References:
[1] Ambrose A M, Christensen H E, Rather L J. Toxicological and pharmacological studies on dihydrorotenone[J]. Journal of the American Pharmaceutical Association (Scientific ed.), 1953, 42(6): 364-366.
[2] Talpade D J, Greene J G, Higgins Jr D S, et al. In vivo labeling of mitochondrial complex I (NADH: ubiquinoneoxidoreductase) in rat brain using [3H] dihydrorotenone[J]. Journal of neurochemistry, 2000, 75(6): 2611-2621.
[3] Greenamyre J T, Higgins D S, Eller R V. Quantitative autoradiography of dihydrorotenone binding to complex I of the electron transport chain[J]. Journal of neurochemistry, 1992, 59(2): 746-749.
[4] Zhang J, Tang J, Cao B, et al. The natural pesticide dihydrorotenone induces human plasma cell apoptosis by triggering endoplasmic reticulum stress and activating p38 signaling pathway[J]. PloS one, 2013, 8(7): e69911.
[5] Xu X, Zhang J, Han K, et al. Natural pesticide dihydrorotenone arrests human plasma cancer cells at the G0/G1 phase of the cell cycle[J]. Journal of Biochemical and Molecular Toxicology, 2014, 28(5): 232-238.
[6] Lee E, Yeo S Y, Lee K W, et al. New screening system using Twist1 promoter activity identifies dihydrorotenone as a potent drug targeting cancer-associated fibroblasts[J]. Scientific Reports, 2020, 10(1): 7058.
Dihydrorotenone是一种杀虫剂，是线粒体复合物I的不可逆抑制剂，并且能够穿过血脑屏障[1]。Dihydrorotenone结合并抑制电子传递链中的复合物I，从而抑制线粒体功能并减少ATP的产生[2]。Dihydrorotenone可被标记用于放射自显影，以研究复合物I在大脑中的独特分布[3]。
在体外，使用20µM的Dihydrorotenone处理24小时，引发了内质网应激并激活了p38信号通路，导致KMS11细胞凋亡[4]。使用15µM的Dihydrorotenone处理24小时，抑制了细胞周期蛋白的表达，导致LP1细胞停滞在G0/G1期，并降低了AKT和ERK的磷酸化水平[5]。使用1µM的Dihydrorotenone处理2周后，SCAF#36细胞中FSP1、PDGFRα和PDGFRβ的表达显著下降，促炎细胞因子基因的表达显著下调，细胞活力明显降低[6]。
| Cell experiment [1]: | |
Cell lines | KMS11 cells |
Preparation Method | KMS11 cells were cultured in DMEM medium supplemented with 10% fetal bovine serum (FBS) and antibiotics (penicillin 100U/ml, streptomycin 0.1mg/ml) in an incubator humidified with 95% air and 5% CO2 at 37°C. KMS11 cells were cultured in 96-well plates at a density of 1.5×104 cells per well and treated with 0, 0.39, 0.78, 1.56, 3.12, 6.25, 12.5, and 25µM of Dihydrorotenone. After incubation for 72 hours, the cell viability was detected. |
Reaction Conditions | 0, 0.39, 0.78, 1.56, 3.12, 6.25, 12.5, and 25µM; 72h |
Applications | Dihydrorotenone treatment decreased the cell viability of KMS11 cells in a dose-dependent manner. |
References: | |
| Cas No. | 6659-45-6 | SDF | |
| 别名 | 二氢鱼藤酮 | ||
| Canonical SMILES | O=C1[C@]2([H])[C@](COC3=CC(OC)=C(OC)C=C32)([H])OC4=C5C(O[C@@H](C(C)C)C5)=CC=C14 | ||
| 分子式 | C23H24O6 | 分子量 | 396.43 |
| 溶解度 | DMSO : 25 mg/mL (63.06 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5225 mL | 12.6126 mL | 25.2251 mL |
| 5 mM | 504.5 μL | 2.5225 mL | 5.045 mL |
| 10 mM | 252.3 μL | 1.2613 mL | 2.5225 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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