Gliquidone

Gliquidone is a second generation sulfonylurea that selectively inhibits ATP-sensitive potassium channel currents (IKATP) in pancreatic beta-cells (IC50s = 0.45, 119.1, and 149.7 µM for HIT-T15 cells, cardiomyocytes, and vascular smooth muscle cells, respectively). It is also a peroxisome proliferator-activated receptor gamma (PPARgamma) agonist (EC50 = 10 µM in a transactivation assay). Gliquidone (0.2 nmol/g) decreases plasma levels of D-glucose and stimulates insulin release in anesthetized rats. It decreases blood glucose levels, serum alkaline phosphatase (ALP), aspartate aminotransferase (AST), and alanine aminotransferase (ALT) activities, and hepatic lipid peroxidation and increases hepatic glutathione (GSH) levels in a rat model of diabetes induced by streptozotocin (STZ, Cay-13104) when administered at a dose of 10 mg/kg.Formal Name: N-[(cyclohexylamino)carbonyl]-4-[2-(3,4-dihydro-7-methoxy-4,4-dimethyl-1,3-dioxo-2(1H)-isoquinolinyl)ethyl]-benzenesulfonamide. CAS Number: 33342-05-1. Synonyms: AR-DF 26. Molecular Formula: C27H33N3O6S. Formula Weight: 527.6. Purity: >98%. 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, Ethanol: 1 mg/ml. lambdamax: 224 nm. SMILES: O=C(N1CCC2=CC=C(S(NC(NC3CCCCC3)=O)(=O)=O)C=C2)C4=CC(OC)=CC=C4C(C)(C)C1=O. InChi Code: InChI=1S/C27H33N3O6S/c1-27(2)23-14-11-20(36-3)17-22(23)24(31)30(25(27)32)16-15-18-9-12-21(13-10-18)37(34,35)29-26(33)28-19-7-5-4-6-8-19/h9-14,17,19H,4-8,15-16H2,1-3H3,(H2,28,29,33). InChi Key: LLJFMFZYVVLQKT-UHFFFAOYSA-N.