| Name | GSK1292263 |
| Description | GSK1292263 is a GPR119 agonist and has been investigated for the treatment of DIABETES MELLITUS, TYPE 2. |
| 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. |
| 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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 32 mg/mL (70.1 mM)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
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| Keywords | diabetes | type | mellitus | GSK 1292263 | GPR119 | inhibit | G Protein-Coupled Receptor 119 | T2DM | Inhibitor | GSK-1292263 | GSK1292263 |
| Inhibitors Related | Vincamine | Monomethyl fumarate | Questiomycin A | 3-Hydroxyoctanoic Acid | CRTh2 antagonist 2 | Fezagepras sodium | Benzyl nicotinate | 1-methoxycyclopropanecarboxylic acid | TUG-1375 | CAY10595 | Timapiprant | NF-56-EJ40 |
| Related Compound Libraries | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Anti-Obesity Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Endocrinology-Hormone Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library |
United States
