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GSK1292263

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Catalog No. T2701Cas No. 1032823-75-8

GSK1292263 is a GPR119 agonist and has been investigated for the treatment of DIABETES MELLITUS, TYPE 2.

GSK1292263

GSK1292263

😃Good
Purity: 99.53%
Catalog No. T2701Cas No. 1032823-75-8
GSK1292263 is a GPR119 agonist and has been investigated for the treatment of DIABETES MELLITUS, TYPE 2.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
2 mg$29In StockIn Stock
5 mg$46In StockIn Stock
10 mg$76In StockIn Stock
25 mg$133In StockIn Stock
50 mg$221In StockIn Stock
100 mg$319-In Stock
1 mL x 10 mM (in DMSO)$48In 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:99.53%
Color:White
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Product Introduction

Bioactivity
Description
GSK1292263 is a GPR119 agonist and has been investigated for the treatment of DIABETES MELLITUS, TYPE 2.
In vitro
In male Sprague-Dawley rats, GSK-1292263 (3-30 mg/kg) was associated with increased levels of gastrointestinal peptides, including glucagon-like peptide 1, oxyntomodulin, peptide YY, and glucagon, especially in the absence of nutrients. This increase was further enhanced by oral glucose administration during glucose tolerance tests. In a 6-week study on Zucker diabetic fatty rats, GSK-1292263 led to a statistically significant increase in insulin immunoreactivity in pancreatic sections compared to the blank control. Furthermore, in a hyperinsulinemic-normoglycemic clamp experiment in Sprague-Dawley rats, GSK-1292263 (10/30 mg/kg) stimulated glucagon secretion without raising blood glucose levels when administered 2 hours before insulin injection, in comparison to the vehicle control.
In vivo
Utilizing Hypo1, GSK-1292263 was identified from a pool of 1,538 compounds. The Fit-Value of GSK-1292263 corresponding to Hypo1 and its estimated value were 8.8 and 7.7 nM, respectively.
Kinase Assay
FTase and GGTase I Activity Assay: FTase and GGTase I activities from 60,000×g supernatants of human Burkitt lymphoma (Daudi) cells are assayed. Inhibition studies are performed by determining the ability of Ras CAAX peptidomimetics to inhibit the transfer of [3H]farnesyl and [3H]geranylgeranyl from [3H]farnesylpyrophosphate and [3H]geranylgeranylpyrophosphate to H-Ras-CVLS and H-Ras-CVLL, respectively.
Chemical Properties
Molecular Weight456.56
FormulaC23H28N4O4S
Cas No.1032823-75-8
SmilesCC(C)c1noc(n1)N1CCC(COc2ccc(nc2)-c2ccc(cc2)S(C)(=O)=O)CC1
Relative Density.1.23 g/cm3
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: 32 mg/mL (70.09 mM), Sonication is recommended.
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
In Vivo Formulation
10% DMSO+90% Corn Oil: 2 mg/mL (4.38 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 mM2.1903 mL10.9515 mL21.9029 mL109.5146 mL
5 mM0.4381 mL2.1903 mL4.3806 mL21.9029 mL
10 mM0.2190 mL1.0951 mL2.1903 mL10.9515 mL
20 mM0.1095 mL0.5476 mL1.0951 mL5.4757 mL
50 mM0.0438 mL0.2190 mL0.4381 mL2.1903 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:
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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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