GIP receptor antagonist (IC50 = 2.6μM). Inhibits GIP-stimulated insulin release from pancreatic β cells in vitro. In ob/ob mice, blocks the effects of GIP on insulin release and plasma glucose levels. Also improves intraperitoneal glucose tolerance, insul
PGlu-3-methyl-His-Pro-NH2 TFA enhances binding to pituitary TRH receptors, thereby increasing the stimulation of thyroid-stimulating hormone (TSH) release from the pituitary.
High affinity rat GIP receptor partial agonist (Kd = 13 nM). Increases cAMP accumulation in COS-7 cells transfected with rat GIP receptor, while also acting as a competitive antagonist of GIP.