TB5

Research use only, not for human use.

TB5 is a potent, selective and reversible inhibitor of hMAO-B.

TB5 is a MAO-B inhibitor. TB5 showed the inhibitory activity and selectivity toward hMAO-B, with Ki and SI values of 0.11±0.01 μm and 13.18, respectively. TB5 was found to be nontoxic at 5 and 25 μm, with 95.75 and 84.59 % viability among cells, respectively.

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.

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.

TB5, TB 5, TB-5

Others

Other Targets

hMAO-B

Neurological Disease

——

948841-07-4

336.25

C15H14BrNOS

>98% (HPLC)

In Vitro:?DMSO : 10 mg/mL (29.74 mM)

CN(C)c1ccc(cc1)/C=C/C(=O)c1ccc(s1)Br

(2E)-1-(5-bromothiophen-2-yl)-3-[4-(dimethylamino)phenyl]prop-2-en-1-one

(-20℃)

With Ice Pack

≥ 2 years