GSK1292263 is a novel GPR119 receptor agonist used for the treatment of type 2 diabetes. The predicted EC50 of GSK1292263 against GPR119 in vitro is at the nanomolar range. (1) The GPR119 receptor is a GPCR which is selectively expressed on pancreatic beta cells and intestinal enteroendocrine cells. Agonists to GPR119 stimulate glucose-dependent insulin secretion in vitro and lower an elevated blood glucose level in vivo.(2)

In vivo, GSK1292263 treatment significantly increases in the peak insulin response and insulin AUC(0-15 min) by 30-60% compared with vehicle control in the intravenous glucose tolerance test. This insulin upregulation correlated with a significant increase in the glucose disposal rate. (3)