| 产品描述： | TB5 is a potent, selective and reversible inhibitor of hMAO-B with a Ki value of 0.11±0.01 μM. |
| 靶点： |
Ki: 0.11±0.01 μM (hMAO-B);MAO; MonoamineOxidase |
| 体外研究： |
TB5 and TB8 interacts with the catalytic site of hMAO-B and hMAO-A with a competitive mode of inhibition. TB5 shows the best inhibitory activity and higher selectivity toward hMAO-B, with Ki and SI values of 0.11±0.01μM and 13.18, respectively. hMAO-B inhibition by compound TB5 and hMAO-A inhibition by compound TB8 are completely reversed after 24 h of dialysis. Cytotoxicity studies show TB5 is nontoxic at 5 and 25 μM, resulting in cell viabilities of 95.75% and 84.59 %, respectively. |
| 体内研究： |
Compounds are dissolved in DMSO (5 mg/mL) and diluted with PBS/EtOH (70:30).Kinetic analyses are carried out for TB5 and TB8. A set of Lineweaver–Burk plots are constructed in the absence and presence of various concentrations of compounds TB5 and TC8. The set consists of five graphs, each constructed by measuring MAO-B and MAO-A catalytic rates at different substrate concentrations (0.1-1 μM). The first Lineweaver–Burk plot is constructed in the absence of inhibitor, while the remaining four graphs are constructed in the presence of different concentrations of TB5 and TB8. |
| 参考文献： |
1. Mathew B, Haridas A, Uçar G, Baysal I, Joy M, Mathew GE, Lakshmanan B, Jayaprakash V. Synthesis, Biochemistry, and Computational Studies of Brominated Thienyl Chalcones: A New Class of Reversible MAO-B Inhibitors. ChemMedChem. 2016 Jun 6;11(11):1161-71. doi: 10.1002/cmdc.201600122. PubMed PMID: 27159243. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.974 ml |
14.87 ml |
29.74 ml |
| 5 mM |
0.595 ml |
2.974 ml |
5.948 ml |
| 10 mM |
0.297 ml |
1.487 ml |
2.974 ml |
| 50 mM |
0.059 ml |
0.297 ml |
0.595 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。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京