APD668

GPR119, a glucose-dependent insulinotropic receptor, is a G protein-coupled receptor that is expressed in pancreatic beta-cells and intestinal L-cells. Activation of GPR119 by the endogenous ligands lyso-phosphatidylcholine (Cay-10172) and oleoyl ethanolamide (Cay-90265) increases intracellular cAMP levels and promotes glucose-stimulated insulin secretion. APD668 is a potent agonist of GPR119 (EC50s = 2.7 and 33 nM for human and rat forms, respectively). Chronic dosing with APD668 in Zucker diabetic fatty rats over several weeks significantly reduces blood glucose and glycated hemoglobin levels.Formal Name: 4-[[1-[2-fluoro-4-(methylsulfonyl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-4-yl]oxy]-1-piperidinecarboxylic acid, 1-methylethyl ester. CAS Number: 832714-46-2. Synonyms: JNJ-28630368. Molecular Formula: C21H24FN5O5S. Formula Weight: 477.5. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMF:PBS (pH 7.2) (1:8): 0.1 mg/ml, DMSO: 20 mg/ml. lambdamax: 242, 276 nm. SMILES: CC(C)OC(N1CCC(OC2=NC=NC3=C2C=NN3C4=CC=C(S(C)(=O)=O)C=C4F)CC1)=O. InChi Code: InChI=1S/C21H24FN5O5S/c1-13(2)31-21(28)26-8-6-14(7-9-26)32-20-16-11-25-27(19(16)23-12-24-20)18-5-4-15(10-17(18)22)33(3,29)30/h4-5,10-14H,6-9H2,1-3H3. InChi Key: XTRUQJBVQBUKSQ-UHFFFAOYSA-N.