Mitoquinone mesylate (Mitoquinone methanesulfonate)
(Synonyms: 米托蒽醌甲磺酸盐; MitoQ mesylate; MitoQ10 mesylate) 目录号 : GC31292
Mitoquinone mesylate（Mitoquinone methanesulfonate）是广泛使用的靶向线粒体的抗氧化剂之一。
Cas No.:845959-50-4
Sample solution is provided at 25 µL, 10mM.
Mitoquinone mesylate (Mitoquinone methanesulfonate) is among the widely used antioxidants that target the mitochondria. It was developed to readily penetrate the BBB and neuronal membranes, where it is concentrated into several hundred-folds within the mitochondria where it mediates the local anti-oxidative capacity [1]. Within the ETC, complex II, also known as succinate dehydrogenase, reduces Mitoquinone mesylate ubiquinone moiety to the active antioxidant ubiquinol which scavenges excess ROS [2].
Mitoquinone mesylate (50 nM) reduced 6-OHDA-induced mitochondrial fragmentation, when used in SH-SY5Y cell line. It inhibited mitochondrial fission protein and the translocation of pro-apoptotic protein (Bax) in the mitochondria [3].
Mitoquinone mesylate treatment inhibited the loss of dopaminergic neurons and enhanced behavioral performance, showed neuroprotective effects in mouse models of PD [4]. Mitoquinone mesylate treatment enhanced the fine motor control and reduced markers of oxidative damage in muscles in a Huntington's disease (HD) mouse model [5]. Mitoquinone mesylate reduced white matter injury, improved neurological performance, and decreased motor-evoked potential latency in intracerebral hemorrhagic (ICH) mice [6].
References:
[1]. Murphy M P, Smith R A J. Targeting antioxidants to mitochondria by conjugation to lipophilic cations[J]. Annu. Rev. Pharmacol. Toxicol., 2007, 47: 629-656.
[2]. James A M, Cochemé H M, Smith R A J, et al. Interactions of Mitochondria-targeted and Untargeted Ubiquinones with the Mitochondrial Respiratory Chain and Reactive Oxygen Species: IMPLICATIONS FOR THE USE OF EXOGENOUS UBIQUINONES AS THERAPIES AND EXPERIMENTAL TOOLS. Journal of Biological Chemistry, 2005, 280(22): 21295-21312.
[3]. Solesio M E, Prime T A, Logan A, et al. The mitochondria-targeted anti-oxidant MitoQ reduces aspects of mitochondrial fission in the 6-OHDA cell model of Parkinson's disease[J]. Biochimica et Biophysica Acta (BBA)-Molecular Basis of Disease, 2013, 1832(1): 174-182.
[4]. Pinho B R, Duarte A I, Canas P M, et al. The interplay between redox signalling and proteostasis in neurodegeneration: In vivo effects of a mitochondria-targeted antioxidant in Huntington's disease mice[J]. Free Radical Biology and Medicine, 2020, 146: 372-382.
[5]. Pinho B R, Duarte A I, Canas P M, et al. The interplay between redox signalling and proteostasis in neurodegeneration: In vivo effects of a mitochondria-targeted antioxidant in Huntington's disease mice[J]. Free Radical Biology and Medicine, 2020, 146: 372-382.
[6]. Chen W, Guo C, Jia Z, et al. Inhibition of mitochondrial ROS by MitoQ alleviates white matter injury and improves outcomes after intracerebral haemorrhage in mice[J]. Oxidative medicine and cellular longevity, 2020, 2020.
Mitoquinone mesylate（Mitoquinone methanesulfonate）是广泛使用的靶向线粒体的抗氧化剂之一。它被开发成很容易穿透 BBB 和神经元膜,在那里它在线粒体中浓缩成数百倍,在线粒体中调节局部抗氧化能力 [1]。在 ETC 中,复合物 II（也称为琥珀酸脱氢酶）将甲磺酸丝裂醌泛醌部分还原为活性抗氧化剂泛醇,后者清除过量的 ROS [2]。
当用于 SH-SY5Y 细胞系时,Mitoquinone mesylate (50 nM) 减少了 6-OHDA 诱导的线粒体断裂。抑制线粒体分裂蛋白和促凋亡蛋白（Bax）在线粒体中的转位[3]。
Mitoquinone mesylate 治疗抑制了多巴胺能神经元的损失并增强了行为表现,在 PD 小鼠模型中显示出神经保护作用 [4]。在亨廷顿舞蹈症 (HD) 小鼠模型中,甲磺酸米托醌治疗增强了精细运动控制并减少了肌肉氧化损伤的标志物[5]。甲磺酸米托醌减少了脑出血 (ICH) 小鼠的白质损伤,改善了神经功能,并减少了运动诱发电位潜伏期 [6]。
| Cell experiment [1]: | |
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Cell lines |
HSC-T6 cells |
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Preparation Method |
Mitoquinone mesylate was added directly to the culture medium at final concentrations of 2 µM, 20 µM, 13 µM, 50 nM, or 10 µM, respectively, for 24 h. |
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Reaction Conditions |
2 µM, 20 µM, 13 µM, 50 nM, or 10 µM for 24 hours |
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Applications |
Confocal fluorescence microscopy showed that mitoquinone mesylate treatment reversed fragmented mitochondria in active HSCs to an elongated state. Immunoblot analysis showed significantly downregulated Fis1 and Drp1 after mitoquinone mesylate treatment. |
| Animal experiment [2]: | |
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Animal models |
male Wistar rats |
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Preparation Method |
For pharmacokinetic study, groups of rats (n = 4-5) were administered either an intravenous (IV) dose (5 mg/kg) via the cannula or an oral dose (25 mg/kg) by gavage. |
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Dosage form |
Intravenous injection, 5 mg/kg; oral, 25 mg/kg. |
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Applications |
After oral administration, mitoquinone mesylate was rapidly absorbed giving a plasma concentration of about 25 ng/mL after about 1 h. Thereafter, mitoquinone mesylate concentration fluctuated reaching a maximum (Cmax) of 31.2 ± 6.9 ng/mL at 4.0 h. After IV administration, the plasma concentration of mitoquinone mesylate exhibited an exponential decline with a rapid distribution phase followed by a slower elimination phase |
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References: [1]: Zhou Y, Long D, Zhao Y, et al. Oxidative stress-mediated mitochondrial fission promotes hepatic stellate cell activation via stimulating oxidative phosphorylation[J]. Cell death & disease, 2022, 13(8): 1-15. |
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| Cas No. | 845959-50-4 | SDF | |
| 别名 | 米托蒽醌甲磺酸盐; MitoQ mesylate; MitoQ10 mesylate | ||
| Canonical SMILES | [O-]S(=O)(C)=O.O=C(C(CCCCCCCCCC[P+](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)=C4C)C(OC)=C(OC)C4=O | ||
| 分子式 | C38H47O7PS | 分子量 | 678.81 |
| 溶解度 | DMSO : 50 mg/mL (73.66 mM);Water : < 0.1 mg/mL (insoluble) | 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 | 1.4732 mL | 7.3658 mL | 14.7317 mL |
| 5 mM | 0.2946 mL | 1.4732 mL | 2.9463 mL |
| 10 mM | 0.1473 mL | 0.7366 mL | 1.4732 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
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Related Biological Data
MitoQ attenuated NLRP3-inflammasome activation and apoptosis in AlCl3-treated Parkin-/- mice hippocampus. (C) Effects of MitoQ on the apoptosis of mice hippocampus by TUNEL staining. The histogram represents the ratio of TUNEL-positive cells.
The second-time was treated with normal saline, MitoQ (5mg/kg body weight, twice weekly，GLPBIO, USA) or MCC950 by intraperitoneal injection in the afternoon of the same day.
Ecotox Environ Safe, 2023, 264: 115459. PMID: 37703808 IF: 6.7996 -
Related Biological Data
MitoQ alleviated mtROS overproduction, activation of NLRP3-inflammasome and W/β signaling, fibrosis and structural and functional damage in the T-2 animal model. (F, G) Protein levels of NLRP3, pro-IL-1β, and caspase-1 p20 in mice kidneys.
MitoQ (100μM, GLPBIO, USA), MCC950 (10μM), or ICG-001 (10μM) were added to the culture medium for 4h before exposing to T-2 media.
J Agr Food Chem (2022). PMID: 36239691 IF: 5.8954 -
Related Biological Data
(J) TUNEL staining of apoptosis.
The MitoQ (GLPBIO, USA) was intraperitoneally administered to mice in HFPO-TA + MitoQ group (5mg/kg, twice/week for 4 weeks).
Food Chem Toxicol (2023): 113706. PMID: 36871880 IF: 5.5716 -
Related Biological Data
ApoE4 exacerbates oxidative stress after oxyHb or SAH. (N-R) Western blots bands (N) of CD16, CD86, Arg-1 and CD206 in APOE4-PBS and APOE4-mitoQ, densitometric quantification of CD16 (O), CD86 (P), Arg-1 (Q) and CD206 (R).
Mitoquinone (GLPBIO, USA) was prepared by dissolving 5mg in dimethylsulfoxide (DMSO).
Neuroscience, 2023. PMID: 37290684 IF: 3.708