An antagonist of GHS-Ra (Ki = 0.017 µM), is selective for GHS-Ra over the motilin receptor (Ki = 6 µM) and a panel of 30 receptors and enzymes (Kis = > 10 µM), prevents ghrelin-induced decreases in insulin secretion in glucose-stimulated isolated rat pancreatic islets at concentration of 1 µM, increases plasma...

Description: YIL 781 is a selective ghrelin receptor antagonist (GHS-R1a) (Ki = 17 nM), showing a weak affinity for kinesin receptors (K = 6 µM). YIL 781 improves glucose homeostasis in vivo and in vitro by blocking ghrelin secretion. Target: GHSR. Smiles:...