MSDC 0160 (Mitoglitazone) 是调节噻唑烷二酮的线粒体靶标 (mTOT) 的胰岛素增敏剂,也是线粒体丙酮酸载体 (MPC) 的调节剂。MSDC 0160 是一种噻唑烷二酮 (TZD),具有抗糖尿病和神经保护活性作用。MSDC 0160 具有用于阿尔茨海默氏病的潜力。
生物活性 | MSDC 0160 (Mitoglitazone) is a mitochondrial target of thiazolidinediones (mTOT)-modulatinginsulinsensitizerand a modulator ofmitochondrial pyruvate carrier (MPC). MSDC 0160 is a thiazolidinedione (TZD) with antidiabetic and neuroprotective activities. MSDC 0160 has the potential for Alzheimer′s disease[1][2]. |
体外研究 (In Vitro) | MSDC 0160 (Mitoglitazone; 1-50 μM; for 24 hours) significantly decreases phosphorylation of mTOR at 20 and 50 μM[1]. MSDC 0160 acts as insulin sensitizers without activating PPARγ[1]. MSDC 0160 (10 μM; pretreatment 1 hour) prevents the MPP+(10 μM)-induced loss of both tyrosine hydroxylase (TH)-immunoreactive differentiated Lund human mesencephalic (LUHMES) cells[1]. MSDC 0160 (10 or 100 μM) prevents the loss of GFP-fluorescent dopaminergic neurons induced by MPP+(0.75 mM) in nematodes[1]. MSDC 0160 (10-20 μM) in conbination with IGF-1 prevents the loss of insulin content and maintains insulin secretion[1]. MSDC 0160 (1-50 μM) treatment maintains human β-cell phenotype[2].
Western Blot Analysis[1] Cell Line: | Human islets | Concentration: | 1, 10, 20, 50 μM | Incubation Time: | For 24 hours | Result: | Significantly decreased Phosphorylation of mTOR at 20 and 50 μM. |
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体内研究 (In Vivo) | MSDC 0160 (Mitoglitazone; 30 mg/kg; oral gavage; daily; for 7 days) improves locomotor behavior, increases survival of nigral dopaminergic neurons, boosts striatal dopamine levels, and reduces neuroinflammation in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-treated mice[2].
Animal Model: | Ten- to 12-week-old male C57BL/6J mice weighing 24 to 28 g[2] | Dosage: | 30 mg/kg | Administration: | Oral gavage; daily; for 7 days | Result: | Improved locomotor behavior, increased survival of nigral dopaminergic neurons, boosted striatal dopamine levels, and reduced neuroinflammation. |
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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 : 33.33 mg/mL(89.98 mM;Need ultrasonic) 配制储备液 1 mM | 2.6996 mL | 13.4982 mL | 26.9964 mL | 5 mM | 0.5399 mL | 2.6996 mL | 5.3993 mL | 10 mM | 0.2700 mL | 1.3498 mL | 2.6996 mL |
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此方案可获得 ≥ 2.5 mg/mL (6.75 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 (6.75 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.75 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 (6.75 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.75 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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