GSK1292263

SKU: orb1305147

Description

GSK1292263 is a selective agonist of the G-protein coupled receptor 119 (GPR119). It has been studied in preclinical research for its potential to stimulate glucose-dependent insulin secretion, making it a candidate for type 2 diabetes mellitus investigation in both in vitro and in vivo models.

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1032823-75-8
• MW: 456.56
• Purity: 99.76% (May vary between batches)
• Formula: C₂₃H₂₈N₄O₄S
• SMILES: CC(C)c1noc(n1)N1CCC(COc2ccc(nc2)-c2ccc(cc2)S(C)(=O)=O)CC1
• Target: GPCR
• Solubility: Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:32 mg/mL (70.09 mM);10% DMSO+90% Corn Oil:2 mg/mL (4.38 mM)

Bioactivity

• 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.
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GSK 1292263, GSK1292263, GSK-1292263, G Protein-Coupled Receptor 119, GPR119, Inhibitor, mellitus, inhibit, diabetes, T2DM, type

Compound Identifiers

PubChem CID

24996872