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948841-07-4

中文名稱 948841-07-4
英文名稱 TB5
CAS 948841-07-4
分子式 C15H14BrNOS
分子量 336.25
MOL 文件 948841-07-4.mol
更新日期 2024/11/08 11:28:13
948841-07-4 結(jié)構(gòu)式 948841-07-4 結(jié)構(gòu)式

基本信息

中文別名
化合物TB5
英文別名
TB5
TB-5
TB 5
1-(5-Bromo-2-thienyl)-3-[4-(dimethylamino)phenyl]-2-propene-1-one
所屬類別
生物化工:激動(dòng)劑抑制劑

物理化學(xué)性質(zhì)

沸點(diǎn)468.5±45.0 °C(Predicted)
密度1.440±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMF: 33 mg/ml; DMSO: 33 mg/ml; Ethanol: 1 mg/ml
酸度系數(shù)(pKa)4.30±0.24(Predicted)
形態(tài)結(jié)晶固體
顏色White to yellow

常見問題列表

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(diǎn)
TargetValue
MAO-B
()
110 nM(Ki)
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.

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