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Beschreibung

A pyrimidine compound that acts as an effective GPR119 agonist (EC50 = 2.5 µ,M in stimulating cAMP in hGPR119-expressing HEK293 cells) and reportedly exhibits no activity toward beta-adrenergic or GLP-1 receptors. Shown to enhance 16.8 mM glucose-induced insulin secretion from murine MIN-6 beta-cells (mU/20 min = 0.22, 0.29, 0.44, respectively, with 0, 1, 10 µ,M AS1269574) in vitro and improve glucose tolerance in normal mice (26% decrease and 60% increase, respectively, of control blood glucose and insulin AUC0-1h in OGTT, 100 mg/kg, p.o.) without affecting basal blood glucose level in either fed or fasting mice in vivo., A pyrimidine compound that acts as an effective GPR119 agonist (EC50 = 2.5 µ,M in stimulating cAMP in hGPR119-expressing HEK293 cells) and reportedly exhibits no activity toward beta-adrenergic or GLP-1 receptors. Shown to enhance 16.8 mM glucose-induced insulin secretion from murine MIN-6 beta-cells (mU/20 min = 0.44 and 0.22, respectively, with or without 10 µ,M AS1269574) in vitro and improve glucose tolerance in normal mice (100 mg/kg, p.o.) without any significant hypoglycemic effect in vivo.