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化學性質:
規格 | 50 mg 100 mg |
CAS | 94 |
別名 | N/A |
化學名 | N/A |
分子式 | C15H14BrNOS |
分子量 | 336.25 |
溶解度 | DMF: 33 mg/ml,DMSO: 33 mg/ml,Ethanol: 1 mg/ml |
儲存條件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
產品描述:
TB5 is a potent, selective and reversible inhibitor of hMAO-B with a Ki value of 0.11±0.01 μM.
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 Ki 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[1].
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[1].
[1]. Mathew B, et al. 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.
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原創作者:上海莼試生物技術有限公司
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