A potent and selective MAO-B inhibitor (Kis = 110 and 1

TB5 – 25 mg

Brand:
Cayman
CAS:
948841-07-4
Storage:
-20
UN-No:
Non-Hazardous - /

TB5 is a potent and selective monoamine oxidase B (MAO-B) inhibitor with Ki values of 110 and 1,450 nM for MAO-B and MAO-A, respectively.{41031} It interacts with the catalytic site of human MAO-B in a competitive manner. In an enzyme assay, MAO-B activity increases from 37% to 97% following inhibitor washout, indicating TB5 binding is reversible. TB5 also demonstrates permeability in a parallel artificial membrane permeation assay (PAMPA), a model for the blood-brain barrier, and has minimal cytotoxicity (>84% cell viability) in HepG2 cells at a concentrations up to 25 μM.  

 

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Description

A potent and selective MAO-B inhibitor (Kis = 110 and 1,450 nM for MAO-B and MAO-A, respectively); interacts with the catalytic site of human MAO-B in a reversible and competitive manner (activity increases from 37% to 97% following inhibitor washout, indicating TB5 binding is reversible); demonstrates permeability in a PAMPA blood-brain barrier model; has minimal cytotoxicity (>84% cell viability) in HepG2 cells at a concentrations up to 25 μM

Formal name: (2E)-1-(5-bromo-2-thienyl)-3-[4-(dimethylamino)phenyl]-2-propen-1-one

Synonyms: 

Molecular weight: 336.2

CAS: 948841-07-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Neuroscience

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