GSK-1292263

GSK‑1292263 is an orally available small molecule agonist of the G protein-coupled receptor 119 (GPR119), developed by GlaxoSmithKline. It acts as a potent and selective agonist at both rodent and human GPR119 receptors with pEC50 values around 6.8 to 6.9[1][5]. Activation of GPR119 enhances glucose-dependent insulin secretion from pancreatic beta cells and stimulates the release of gut hormones such as GLP‑1, thereby improving glucose tolerance[5][7]. In clinical studies for type 2 diabetes mellitus (T2DM), it was shown to increase insulin secretion in a glucose-sensitive manner and improve metabolic parameters in animal models; however, it did not significantly lower plasma glucose in T2DM patients but showed unexpected lipid-lowering effects including reduced LDL cholesterol and triglycerides with increased HDL cholesterol[6]. The drug reached Phase II clinical trials for type 2 diabetes mellitus and hyperlipidemia but development was discontinued for these indications[7].

Other names

3-Isopropyl-5-(4-(((6-(4-(methylsulfonyl)phenyl)pyridin-3-yl)oxy)methyl)piperidin-1-yl)-1,2,4-oxadiazole(1-(3-isopropyl–1,2,4–oxadiazol–5–yl)piperidin–4–yl)methyl methanesulfonate5-[({1-[3-(1-Methylethyl )–1,2,4–oxadiazol–5-yl]−4-piperidinyl}methyl)oxy]−2-[4-(methylsulfonyl)phenyl]pyridine