A potent and selective MAO-B inhibitor
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TB5

Item No. 22947

Technical Information
Formal Name
(2E)-1-(5-bromo-2-thienyl)-3-[4-(dimethylamino)phenyl]-2-propen-1-one
CAS Number
948841-07-4
Molecular Formula
C15H14BrNOS
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 33 mg/mlDMSO: 33 mg/mlEthanol: 1 mg/ml
λmax
436 nm
SMILES
CN(C)C1=CC=C(/C=C/C(C2=CC=C(Br)S2)=O)C=C1
InChi Code
InChI=1S/C15H14BrNOS/c1-17(2)12-6-3-11(4-7-12)5-8-13(18)14-9-10-15(16)19-14/h3-10H,1-2H3/b8-5+
InChi Key
PTLDLBSWTKNYCY-VMPITWQZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    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.1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Mathew, B., Haridas, A., Uçar, G., et alSynthesis, biochemistry, and computational studies of brominated thienyl chalcones: A new class of reversible MAO-B inhibitors. ChemMedChem 11(11), 1161-1171 (2016).