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

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $29 | In Stock | In Stock | |
| 5 mg | $46 | In Stock | In Stock | |
| 10 mg | $76 | In Stock | In Stock | |
| 25 mg | $133 | In Stock | In Stock | |
| 50 mg | $221 | In Stock | In Stock | |
| 100 mg | $319 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $48 | In Stock | In Stock |
| 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. |
| Molecular Weight | 456.56 |
| Formula | C23H28N4O4S |
| Cas No. | 1032823-75-8 |
| Smiles | CC(C)c1noc(n1)N1CCC(COc2ccc(nc2)-c2ccc(cc2)S(C)(=O)=O)CC1 |
| Relative Density. | 1.23 g/cm3 |
| 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: 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
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Dissolve 2 mg of the compound in 100 μL DMSO
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.
1) Add 100 μL of the DMSO
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
and mix thoroughly until a homogeneous solution is obtained.
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