TB-5

TB-5 - Names and Identifiers

Name	(2E)-1-(5-bromothiophen-2-yl)-3-[4-(dimethylamino)phenyl]prop-2-en-1-one
Synonyms	TB5 TB-5 TB 5 1-(5-Bromo-2-thienyl)-3-[4-(dimethylamino)phenyl]-2-propene-1-one (2E)-1-(5-bromothiophen-2-yl)-3-[4-(dimethylamino)phenyl]prop-2-en-1-one
CAS	948841-07-4

TB-5 - Physico-chemical Properties

Molecular Formula	C15H14BrNOS
Molar Mass	336.25
Solubility	Soluble in DMSO
Storage Condition	-20℃
Use	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.
Target	Ki: 0.11±0.01 μM (hMAO-B)
In vitro study	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.
In vivo study	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.

TB-5 - Reference

Reference

1: Mathew B, Haridas A, Uçar G, Baysal I, Joy M, Mathew GE, Lakshmanan B, Jayaprakash V. 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. doi: 10.1002/cmdc.201600122. PubMed PMID: 27159243.

TB-5 - Preparation solution concentration reference

	1mg	5mg	10mg
1 mM	2.974 ml	14.87 ml	29.74 ml
5 mM	0.595 ml	2.974 ml	5.948 ml
10 mM	0.297 ml	1.487 ml	2.974 ml
5 mM	0.059 ml	0.297 ml	0.595 ml

Last Update：2024-01-02 23:10:35

TB-5 - Reference Information

biological activity	TB5 is a potent, selective MAO-B inhibitor, ki values for MAO-B and MAO-A were 110 nM and 1450 nM, respectively.
Target	Value
MAO-B ()	110 nM(Ki)

Last Update：2024-04-09 02:00:14