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TPA 023

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Catalog No. T17144Cas No. 252977-51-8

TPA 023 is a selective agonist of GABAA α2/α3 subtype (Kis = 0.19 - 0.41 nM).

TPA 023

TPA 023

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Purity: 99.75%
Catalog No. T17144Cas No. 252977-51-8
TPA 023 is a selective agonist of GABAA α2/α3 subtype (Kis = 0.19 - 0.41 nM).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$67In StockIn Stock
5 mg$135In StockIn Stock
10 mg$196-In Stock
25 mg$338-In Stock
50 mg$542-In Stock
1 mL x 10 mM (in DMSO)$148In 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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Purity:99.75%
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Product Introduction

Bioactivity
Description
TPA 023 is a selective agonist of GABAA α2/α3 subtype (Kis = 0.19 - 0.41 nM).
Targets&IC50
GABAA:(ki)0.19-0.41 nM
In vivo
TPA023 (0.7, 2.0, and 5 mg/kg, p.o.) blocks ketamine's cognitive-impairing ability but does not influence the behavioral symptoms of rhesus monkeys[1]. In rats, TPA023 (0.42 mg/kg; oral) displays good receptor occupancy and results in 50% occupancy of rat brain GABAA receptors, with the corresponding plasma concentration being 25 ng/mL. TPA023 (3 mg/kg p.o. in 0.5% methylcellulose) shows anxiolytic-like effect on rats. TPA023(10 mg/kg i.p.) is efficacious in the mouse pentylenetetrazole-induced seizure model, providing full seizure protection(84% occupancy), with the ED50 of 0.19-0.41 nM[2].
Chemical Properties
Molecular Weight395.43
FormulaC20H22FN7O
Cas No.252977-51-8
SmilesCCn1ncnc1COc1nn2c(nnc2cc1C(C)(C)C)-c1ccccc1F
Relative Density.1.33 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: 50 mg/mL (126.44 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.5289 mL12.6445 mL25.2889 mL126.4446 mL
5 mM0.5058 mL2.5289 mL5.0578 mL25.2889 mL
10 mM0.2529 mL1.2644 mL2.5289 mL12.6445 mL
20 mM0.1264 mL0.6322 mL1.2644 mL6.3222 mL
50 mM0.0506 mL0.2529 mL0.5058 mL2.5289 mL
100 mM0.0253 mL0.1264 mL0.2529 mL1.2644 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

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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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