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 |
|
注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |