S80369 |
MSDC 0160 |
源叶(MedMol) | 98% |
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- 产品描述: MSDC 0160 (Mitoglitazone) is a mitochondrial target of thiazolidinediones (mTOT)-modulating insulin sensitizer and a modulator of mitochondrial pyruvate carrier (MPC). MSDC 0160 is a thiazolidinedione (TZD) with antidiabetic and neuroprotective activities. MSDC 0160 has the potential for Alzheimer′s disease
- 靶点: Insulin Receptor;Mitochondrial Metabolism;IGF-1R;MitochondrialMetabolism
- 体外研究:
MSDC 0160 (Mitoglitazone; 1-50 µM; for 24 hours) significantly decreases phosphorylation of mTOR at 20 and 50 µM. MSDC 0160 acts as insulin sensitizers without activating PPARγ. 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. MSDC 0160 (10 or 100 μM) prevents the loss of GFP-fluorescent dopaminergic neurons induced by MPP+ (0.75 mM) in nematodes. MSDC 0160 (10-20 μM) in conbination with IGF-1 prevents the loss of insulin content and maintains insulin secretion. MSDC 0160 (1-50 μM) treatment maintains human β-cell phenotype. Western Blot Analysis 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.
- 体内研究:
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. Animal Model: Ten- to 12-week-old male C57BL/6J mice weighing 24 to 28 g 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.
- 参考文献:
1. Rohatgi N, et al. Novel insulin sensitizer modulates nutrient sensing pathways and maintains β-cell phenotype in human islets. PLoS One. 2013 May 1;8(5):e62012. 2. Ghosh A, et al. Mitochondrial pyruvate carrier regulates autophagy, inflammation, and neurodegeneration inexperimental models of Parkinson's disease. Sci Transl Med. 2016 Dec 7;8(368):368ra174.
- 溶解性: soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.7 ml 13.498 ml 26.996 ml 5 mM 0.54 ml 2.7 ml 5.399 ml 10 mM 0.27 ml 1.35 ml 2.7 ml 50 mM 0.054 ml 0.27 ml 0.54 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)