TB5

生物活性靶點體外研究體內(nèi)研究 用途與合成方法 MSDS TB5價格(試劑級) 上下游產(chǎn)品信息

中文名稱	TB5
中文同義詞	化合物TB5;(E)-1-(5-溴噻吩-2-基)-3-(4-(二甲基氨基)苯基)丙-2-烯-1-酮
英文名稱	TB5
英文同義詞	1-(5-Bromo-2-thienyl)-3-[4-(dimethylamino)phenyl]-2-propene-1-one;TB-5;TB 5;TB5;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號	948841-07-4
分子式	C15H14BrNOS
分子量	336.25
EINECS號
相關(guān)類別
Mol文件	948841-07-4.mol
結(jié)構(gòu)式

TB5 性質(zhì)

TB5 用途與合成方法

生物活性

TB5是一種有效的、選擇性MAO-B抑制劑，對MAO-B和MAO-A的Ki值分別為110 nM和1450 nM。

靶點

體外研究

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.

體內(nèi)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.

安全信息

MSDS信息

TB5 價格(試劑級)

TB5 上下游產(chǎn)品信息