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GSK205

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Catalog No. T11480Cas No. 1263068-83-2

GSK205 is a selective TRPV4 antagonist that blocks Ca(2+) signaling and may be used to reduce inflammation and pain.

GSK205

GSK205

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Purity: 99.46%
Catalog No. T11480Cas No. 1263068-83-2
GSK205 is a selective TRPV4 antagonist that blocks Ca(2+) signaling and may be used to reduce inflammation and pain.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$64In StockIn Stock
5 mg$156In StockIn Stock
10 mg$247In StockIn Stock
25 mg$546In StockIn Stock
50 mg$892In StockIn Stock
100 mg$1,430-In Stock
1 mL x 10 mM (in DMSO)$165In 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:99.46%
Appearance:Solid
Color:Yellow
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Product Introduction

Bioactivity
Description
GSK205 is a selective TRPV4 antagonist that blocks Ca(2+) signaling and may be used to reduce inflammation and pain.
Targets&IC50
TRPV4:4.19  μM
In vitro
In T3-F442A adipocytes, GSK205 (5 μM; 4 days) resulted in increased expression of thermogenic genes and was accompanied by a decrease in the proinflammatory gene program[1].
In vivo
In male C57BL/6J mice on a high-fat diet, GSK205 (10 mg/kg; intraperitoneal injection; twice daily; for 7 days) caused a reduced expression of proinflammatory chemokines, macrophage markers, and Tnfa in EPI fat. It also significantly improved glucose tolerance in diet-induced obese (DIO) mice[1].
Chemical Properties
Molecular Weight481.45
FormulaC24H25BrN4S
Cas No.1263068-83-2
SmilesBr.CN(CCc1ccc(Nc2ncc(s2)-c2cccnc2)cc1)Cc1ccccc1
Relative Density.no data available
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: 100 mg/mL (207.71 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (8.31 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
1mg5mg10mg50mg
1 mM2.0771 mL10.3853 mL20.7706 mL103.8529 mL
5 mM0.4154 mL2.0771 mL4.1541 mL20.7706 mL
10 mM0.2077 mL1.0385 mL2.0771 mL10.3853 mL
20 mM0.1039 mL0.5193 mL1.0385 mL5.1926 mL
50 mM0.0415 mL0.2077 mL0.4154 mL2.0771 mL
100 mM0.0208 mL0.1039 mL0.2077 mL1.0385 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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