TB5

TB5

中文名称TB5
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 结构式

TB5 性质

沸点468.5±45.0 °C(Predicted)
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)

TB5 用途与合成方法

TB5是一种有效的、选择性MAO-B抑制剂,对MAO-B和MAO-A的Ki值分别为110 nM和1450 nM。
TargetValue
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

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/01/25HY-100975TB55 mg500元
2024/01/25HY-100975948841-07-4
TB5
948841-07-410mM * 1mLin DMSO550元

TB5 上下游产品信息

"TB5"相关产品信息
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