中文名 | TB5 |
英文名 | (2E)-1-(5-bromothiophen-2-yl)-3-[4-(dimethylamino)phenyl]prop-2-en-1-one |
别名 | 化合物TB5 |
英文别名 | TB5 TB-5 TB 5 1-(5-Bromo-2-thienyl)-3-[4-(dimethylamino)phenyl]-2-propene-1-one (2E)-1-(5-bromothiophen-2-yl)-3-[4-(dimethylamino)phenyl]prop-2-en-1-one |
CAS | 948841-07-4 |
化学式 | C15H14BrNOS |
分子量 | 336.25 |
溶解度 | 溶于DMSO |
存储条件 | -20℃ |
靶点 | Ki: 0.11±0.01 μM (hMAO-B) |
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 K i 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. |
参考资料 展开查看 | 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. |
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 |
5 mM | 0.059 ml | 0.297 ml | 0.595 ml |
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