GPR39-C3

GPR39-C3 is a potent agonist of the orphan G protein-coupled receptor GPR39 with EC50 values of 0.8 and 0.4 nM for cAMP production in HEK293 cells expressing human and rat receptors, respectively. It is selective for GPR39 over a panel of kinases (IC50s = >10 µM), ghrelin and neurotensin-1 receptors (IC50s = >30 µM), and a variety of enzymes, transporters, or G protein-coupled receptors. GPR39-C3 increases secretion of glucagon-like peptide 1 (GLP-1, Cay-24460) in STC-1 mouse enteroendocrine cells (EC50 = 0.06 µM) and is protective against cytokine-induced cell death in INS-1E rat insulinoma cells (EC50 = 0.02 µM). In vivo, GPR39-C3 (30 mg/kg) increases the amount of active GLP-1 in sera by 6-fold in glucose-challenged mice when administered concurrently with a dipeptidyl peptidase 4 (DPP-4) inhibitor.Formal Name: N-[3-chloro-4-[[[2-(methylamino)-6-(2-pyridinyl)-4-pyrimidinyl]amino]methyl]phenyl]-methanesulfonamide. CAS Number: 1621175-65-2. Molecular Formula: C18H19ClN6O2S. Formula Weight: 418.9. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2)(1:5): 0.16 mg/ml. lambdamax: 229, 331 nm. SMILES: CS(NC1=CC=C(CNC2=NC(NC)=NC(C3=CC=CC=N3)=C2)C(Cl)=C1)(=O)=O. InChi Code: InChI=1S/C18H19ClN6O2S/c1-20-18-23-16(15-5-3-4-8-21-15)10-17(24-18)22-11-12-6-7-13(9-14(12)19)25-28(2,26)27/h3-10,25H,11H2,1-2H3,(H2,20,22,23,24). InChi Key: DRSZMILOMUPIBJ-UHFFFAOYSA-N.