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TB5
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TB5图片
CAS NO:948841-07-4
规格:≥98%
包装与价格:
包装价格(元)
2mg电议
5mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 336.25
Formula C15H14BrNOS
CAS No. 948841-07-4
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 10mM
Water: N/A
Ethanol: N/A
Chemical Name (2E)-1-(5-bromothiophen-2-yl)-3-[4-(dimethylamino)phenyl]prop-2-en-1-one
Synonyms TB5, TB 5, TB-5
SMILES Code O=C(C1=CC=C(Br)S1)/C=C/C2=CC=C(N(C)C)C=C2
实验参考方法
In Vitro

In vitro activity: TB5 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.


Kinase Assay: 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


Cell Assay: In vitro cytotoxicity of brominated thiophene chalcones and standard MAO inhibitors are tested in human HepG2 hepatic cancer cells at three different concentrations (1, 5 and 25 μM).

In VivoTest 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
Animal model
Formulation & Dosage 5 mg/mL
References ChemMedChem. 2016 Jun 6;11(11):1161-71.