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A2AAR antagonist 3

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Catalog No. T211007

A2AAR antagonist 3 is a potent and selective A2A adenosine receptor (A2AAR) antagonist with an IC50 value of 1.57 nM. It exhibits a high binding affinity specifically for A2AAR. In vitro studies demonstrate its good stability in rat liver microsomes, and it possesses acceptable pharmacokinetic properties in vivo. A2AAR antagonist 3 is applicable for cancer research.

A2AAR antagonist 3

A2AAR antagonist 3

😃Good
Catalog No. T211007
A2AAR antagonist 3 is a potent and selective A2A adenosine receptor (A2AAR) antagonist with an IC50 value of 1.57 nM. It exhibits a high binding affinity specifically for A2AAR. In vitro studies demonstrate its good stability in rat liver microsomes, and it possesses acceptable pharmacokinetic properties in vivo. A2AAR antagonist 3 is applicable for cancer research.
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Product Introduction

Bioactivity
Description
A2AAR antagonist 3 is a potent and selective A2A adenosine receptor (A2AAR) antagonist with an IC50 value of 1.57 nM. It exhibits a high binding affinity specifically for A2AAR. In vitro studies demonstrate its good stability in rat liver microsomes, and it possesses acceptable pharmacokinetic properties in vivo. A2AAR antagonist 3 is applicable for cancer research.
In vitro
A2AAR antagonist 3 (Compound 12a) at a concentration of 1 μM over 48 hours can restore IL-2 secretion in human peripheral blood mononuclear cells inhibited by NECA (1 μM, pretreated for 30 minutes). Furthermore, A2AAR antagonist 3, within a range of 3.125-100 μM over 24 hours, shows no significant toxicity to L929, H9C2, and HTX2426 cells.
Chemical Properties
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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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:
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2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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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
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