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GSK682753A

Name: GSK682753A
Brand: TargetMol
SKU: T11498
Rating: 4.5 (1 reviews)

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Catalog No. T11498Cas No. 1334294-76-6

GSK682753A is a selective and highly potent inverse agonist of the Epstein-Barr virus-induced receptor 2 (EBI2) with an IC50 of 53.6 nM.

GSK682753A

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Catalog No. T11498Cas No. 1334294-76-6

GSK682753A is a selective and highly potent inverse agonist of the Epstein-Barr virus-induced receptor 2 (EBI2) with an IC50 of 53.6 nM.

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
2 mg	$95	5 days	5 days

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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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Product Introduction

Bioactivity

Description	GSK682753A is a selective and highly potent inverse agonist of the Epstein-Barr virus-induced receptor 2 (EBI2) with an IC50 of 53.6 nM.
Targets&IC50	EBI2/GPR183:53.6 nM
In vitro	GSK682753A exhibits dose-dependent inhibition of EBI2, achieving an IC50 of 53.6 nM. It demonstrates similar potency in inhibiting ERK phosphorylation, GTPγS binding, and activation of the cAMP-response element-binding protein (CREB). Additionally, GSK682753A acts as a selective and highly potent inverse agonist for both murine and human EBI2, effectively blocking G protein-dependent and potentially G protein-independent signals. In assays using cAMP-response element-binding protein-based reporters and guanosine 5'-3-O-(thio)-triphosphate (GTPγS) binding, GSK682753A shows a potency range of 2.6-53.6 nM and achieves an inhibitory efficacy of 75%.

Chemical Properties

Molecular Weight	479.78
Formula	C₂₃H₂₁Cl₃N₂O₃
Cas No.	1334294-76-6
Smiles	Clc1ccc(\C=C\C(=O)N2CCC3(CN(Cc4ccc(Cl)c(Cl)c4)C(=O)O3)CC2)cc1
Relative Density.	1.44 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 27 mg/mL (56.28 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Corn Oil: 2 mg/mL (4.17 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0843 mL	10.4214 mL	20.8429 mL	104.2144 mL
5 mM	0.4169 mL	2.0843 mL	4.1686 mL	20.8429 mL
10 mM	0.2084 mL	1.0421 mL	2.0843 mL	10.4214 mL
20 mM	0.1042 mL	0.5211 mL	1.0421 mL	5.2107 mL
50 mM	0.0417 mL	0.2084 mL	0.4169 mL	2.0843 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:

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 DMSO TargetMol | 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 DMSO TargetMol | reagent stock solution to 400 μL PEG300 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 ddH₂O TargetMol | 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.

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