TB5
中文名称 | TB5 |
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中文同义词 | 化合物TB5 |
英文名称 | TB5 |
英文同义词 | TB5;1-(5-Bromo-2-thienyl)-3-[4-(dimethylamino)phenyl]-2-propene-1-one;TB-5;TB 5;MAO,TB-5,Monoamine Oxidase,TB 5,TB5,Inhibitor,inhibit;2-Propen-1-one, 1-(5-bromo-2-thienyl)-3-[4-(dimethylamino)phenyl]-, (2E)- |
CAS号 | 948841-07-4 |
分子式 | C15H14BrNOS |
分子量 | 336.25 |
EINECS号 | |
相关类别 | |
Mol文件 | 948841-07-4.mol |
结构式 |
TB5 性质
沸点 | 468.5±45.0 °C(Predicted) |
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密度 | 1.440±0.06 g/cm3(Predicted) |
储存条件 | Store at -20°C |
溶解度 | DMF:33mg/mL; DMSO:33mg/mL;乙醇:1mg/mL |
形态 | 结晶固体 |
酸度系数(pKa) | 4.30±0.24(Predicted) |
Target | Value |
MAO-B
() | 110 nM(Ki) |
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.
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.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024/01/25 | HY-100975 | TB5 | 5 mg | 500元 | |
2024/01/25 | HY-100975 | 948841-07-4 TB5 | 948841-07-4 | 10mM * 1mLin DMSO | 550元 |