| 名称 | MSDC 0160 |
| 描述 | MSDC 0160 (CAY10415) is a prototype mTOT-modulating insulin sensitizer being used in trials studying the treatment of Type 2 Diabetes and Alzheimer's Disease. |
| 激酶实验 | Measurement of activities of autophosphorylated/non-autophosphorylate CaMKII: CaMKII activity is measured utilizing syntideII as a substrate. Purified CaMKII is pre-incubated in the assay mixture ( 35 mM Hepes-Na ( pH 8.0 ), 10 mM MgC12, 0.5 μM CaM, 5 μM ATP, 1 mM CaCl2 or 1 mM EGTA, total 25 μL) at 30 °C for 2 minutes. After this pre-incubation, the protein substrate/radioactive ATP mixture is added to the same test tube and the preparation is further incubated at 30 °C, for 5 minutes ( final assay condition; 35 mM Hepes-Na (pH 8.0), 10 mM MgCl2, 0.125 μM CaCl2, 20 μM syntideII, 11.25 μM [ γ-32P] ATP, 10 % DMSO and indicated concentrations of KN-93, supplemented with 0.25 mM CaCl2 and 2 mM EGTA (for autophosphorylated samples) or 0.25 mM EGTA and 2 mM CaCl2 (for nonautophosphorylated samples ), total 100 μL ). The reaction is terminated by adding of 25 μL of 100 % ( w/v ) ice-cold TCA. After centrifugation, 80 μL of the supernatant is applied to phosphocellulose paper. The filters are then washed with 75 mM H3P04 for 15 min with continuous agitation. After 4-cycles of washing, the radioactivity retains on the filter paper is quantified in a liquid scintillation counter. |
| 体外活性 | 在糖尿病的KKAy小鼠模型中,通过大量减少循环系统中的胰岛素和葡萄糖,MSDC-0160（100 mg/kg,p.o.）使胰岛素的敏感性提高. |
| 体内活性 | 在胰岛素和IGF-1信号通路中,MSDC-0160可降低抗性,使IGF-1诱导的AKt和GSK-3磷酸化恢复。MSDC-0160与IGF-1及8 mM葡萄糖联用增加β细胞中特定基因的表达,包括胰岛素,pdx1,nkx6.1及nkx2.2,并维持胰岛素含量但对葡萄糖诱导的胰岛素分泌无影响。此外,MSDC-0160对人β细胞分化有促进作用,并减少凋亡标志物表达。 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.4 mM), Sonication is recommended.
DMSO : 37 mg/mL (99.89 mM), Sonication is recommended.
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| 关键字 | thiazolidinedione | sensitizer | pyruvate | neuroprotective | mTOT | MSDC 0160 | MPC | MitochondrialMetabolism | Mitochondrial Metabolism | mitochondrial | Insulin Receptor | insulin | Inhibitor | inhibit | IGF1R | CAY-10415 | CAY 10415 | carrier | antidiabetic | Alzheimer |
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