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TB5

😃Good
Catalog No. T3596Cas No. 948841-07-4

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

TB5

TB5

😃Good
Purity: 99.61%
Catalog No. T3596Cas No. 948841-07-4
TB5 is a potent, selective, and reversible inhibitor of hMAO-B.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mg$41In StockIn Stock
10 mg$66In StockIn Stock
25 mg$121In StockIn Stock
50 mg$197In StockIn Stock
100 mg$316-In Stock
1 mL x 10 mM (in DMSO)$45In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Batch Information

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Purity:99.61%
Appearance:Solid
Color:Yellow
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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/Shipping at ambient temperature.
Solubility Information
DMSO: 55 mg/mL (163.57 mM), Sonication is recommended.
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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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

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