Formulation: A crystalline solid
Formal Name: 4-[[5-methoxy-6-[[2-methyl-6-(methylsulfonyl)-3-pyridinyl]amino]-4-pyrimidinyl]oxy]-1-piperidinecarboxylic acid, 1-methylethyl ester
Purity: ≥98%
Formula Markup: C21H29N5O6S
Formula Weight: 479,6
Shelf life (days): 1460
CAS Number: 897732-93-3
Notes: APD597 is an orally bioavailable agonist of GPR119 that has EC50 values of 46 and 421 nM for the human and rat receptors, respectively, in a homologous time-resolved fluorescence (HTRF) assay.{48588} It increases insulin secretion stimulated by a high, but not low, concentration of glucose in isolated mouse pancreatic β-cells and in isolated human islets.{48589} APD597 (20 mg/kg) increases levels of glucagon-like peptide-1 (GLP-1; Item No. 24460) induced by glucose in mice. It also decreases blood glucose levels in an oral glucose tolerance test in mice when administered at doses of 1 and 10 mg/kg and in Zucker diabetic rats at a dose of 3 mg/kg.{48588}