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GSK0660

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Catalog No. T2674Cas No. 1014691-61-2

GSK0660 is an antagonist and inverse agonist of PPARβ/δ.

GSK0660

GSK0660

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Purity: 99.70%
Catalog No. T2674Cas No. 1014691-61-2
GSK0660 is an antagonist and inverse agonist of PPARβ/δ.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
2 mg$39In StockIn Stock
5 mg$63In StockIn Stock
10 mg$106In StockIn Stock
25 mg$195In StockIn Stock
50 mg$388In StockIn Stock
100 mg$577In StockIn Stock
500 mg$1,260-In Stock
1 mL x 10 mM (in DMSO)$63In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.70%
Color:White to Yellow
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Product Introduction

Bioactivity
Description
GSK0660 is an antagonist and inverse agonist of PPARβ/δ.
Targets&IC50
PPARβ/δ:155 nM
Kinase Assay
Human astrocytoma cells, 1321N1, are grown to stably express rat P2X7, human P2X4, P2X2a, P2X2/3, P2X1, P2Y1?and P2Y2 recombinant receptors. Agonist, BzATP, 2,3-O-(4-ben-zoylbenzoyl)-ATP or ATP-induced changes in intracellular Ca2+?concentrations are assessed in all of the cell lines using the Ca2+?chelating dye, Fluo-4, in conjunction with a Fluorometric Imaging Plate Reader. The cells are plated out the day before the experiment onto poly-D-lysine-coated black 96 well plates. After the agonist addition, changes in intracellular Ca2+ concentrations are recorded, per second, for 3 min. Ligands are tested at 11 half-log concentrations from 10-10 to 10-4 M. BzATP or ATP concentrations corresponds to the EC70?values for each receptor to enable comparison of antagonist potencies across the multiple P2 receptor subtypes. A 438079 is added to the cell plate and ?uorescence data are collected for 3 min before the addition of agonist, subsequently, data are then collected for another 2 min. The pEC50 or pIC50 values are derived from a single curve ?t.
Chemical Properties
Molecular Weight418.49
FormulaC19H18N2O5S2
Cas No.1014691-61-2
SmilesS(NC1=C(OC)C=C(NC2=CC=CC=C2)C=C1)(=O)(=O)C3=C(C(OC)=O)SC=C3
Relative Density.1.413 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
Ethanol: 4.19 mg/mL (10.01 mM), Sonication is recommended.
DMSO: 117.5 mg/mL (280.77 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.78 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
Ethanol/DMSO
1mg5mg10mg50mg
1 mM2.3895 mL11.9477 mL23.8954 mL119.4772 mL
5 mM0.4779 mL2.3895 mL4.7791 mL23.8954 mL
10 mM0.2390 mL1.1948 mL2.3895 mL11.9477 mL
DMSO
1mg5mg10mg50mg
20 mM0.1195 mL0.5974 mL1.1948 mL5.9739 mL
50 mM0.0478 mL0.2390 mL0.4779 mL2.3895 mL
100 mM0.0239 mL0.1195 mL0.2390 mL1.1948 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

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