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TB5

🥰Excellent
Catalog No. T3596Cas No. 948841-07-4

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

TB5

TB5

🥰Excellent
Purity: 99.82%
Catalog No. T3596Cas No. 948841-07-4
TB5 is a potent, selective, and reversible inhibitor of hMAO-B.
Pack SizePriceAvailabilityQuantity
5 mg$41In Stock
10 mg$66In Stock
25 mg$121In Stock
50 mg$197In Stock
100 mg$316In Stock
1 mL x 10 mM (in DMSO)$45In Stock
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Purity:99.82%
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Product Introduction

Bioactivity
Description
TB5 is a potent, selective, and reversible inhibitor of hMAO-B.
Targets&IC50
MAO-B (human):0.11±0.01 μM. (Ki)
In vitro
TB5 and TB8 interact competitively with the catalytic sites of hMAO-B and hMAO-A. TB5 shows the highest inhibitory activity and selectivity toward hMAO-B, with Ki and SI values of 0.11±0.01 μM and 13.18, respectively. Inhibition by TB5 (hMAO-B) and TB8 (hMAO-A) is fully reversible after 24 hours of dialysis. Cytotoxicity studies reveal TB5 is non-toxic at 5 and 25 μM, with cell viabilities of 95.75% and 84.59%, respectively [1].
In vivo
Compounds are initially dissolved in DMSO (5 mg/mL), then further diluted with a PBS/EtOH mixture (70:30). To elucidate the critical interactions dictating selectivity and potency, kinetic analyses of TB5 and TB8 are conducted. Lineweaver–Burk plots, a total of five, are created to compare the catalytic rates of MAO-B and MAO-A at various substrate concentrations (0.1-1 μM) in both the absence and presence of TB5 and TB8 at differing concentrations. The initial plot reveals the baseline enzyme activity without inhibitors, while the subsequent four plots show the impact of varying concentrations of TB5 and TB8[1].
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[1].
Cell Research
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)[1].
Chemical Properties
Molecular Weight336.25
FormulaC15H14BrNOS
Cas No.948841-07-4
SmilesCN(C)c1ccc(\C=C\C(=O)c2ccc(Br)s2)cc1
Relative Density.1.440 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 55 mg/mL (163.57 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.9740 mL14.8699 mL29.7398 mL148.6989 mL
5 mM0.5948 mL2.9740 mL5.9480 mL29.7398 mL
10 mM0.2974 mL1.4870 mL2.9740 mL14.8699 mL
20 mM0.1487 mL0.7435 mL1.4870 mL7.4349 mL
50 mM0.0595 mL0.2974 mL0.5948 mL2.9740 mL
100 mM0.0297 mL0.1487 mL0.2974 mL1.4870 mL

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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