Gliclazide

Gliclazide is a sulfonylurea and an inhibitor of pancreatic beta-cell ATP-sensitive potassium (KATP) channels (IC50 = 184 nM for murine beta-cells). It is selective for pancreatic beta-cell over cardiac and arterial smooth muscle cell KATP channels (IC50s = 19.5 and 37.9 µM, respectively). Gliclazide (5 µM) increases insulin-induced glucose uptake and glucose transporter 4 (GLUT4) translocation to the plasma membrane in a differentiated 3T3L1 adipocyte model of insulin resistance induced by hydrogen peroxide. Gliclazide (5 and 10 µg/ml) reduces LDL oxidation by human aortic smooth muscle cells (HASMCs), decreasing TBARS content and 8-isoprostane levels. It also decreases oxidized LDL-induced HASMC proliferation and monocyte adhesion when used at concentrations ranging from 1 to 10 µg/ml. Gliclazide (5 mg/kg) reduces serum glucose levels and increases glucose uptake by isolated rat hindquarters in a model of diabetes induced by streptozotocin (STZ, Cay-13104).Formal Name: N-[[(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)amino]carbonyl]-4-methyl-benzenesulfonamide. CAS Number: 21187-98-4. Molecular Formula: C15H21N3O3S. Formula Weight: 323.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml, DMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml, Ethanol: slightly soluble. lambdamax: 230, 310 nm. SMILES: CC1=CC=C(S(NC(NN2CC3C(CCC3)C2)=O)(=O)=O)C=C1. InChi Code: InChI=1S/C15H21N3O3S/c1-11-5-7-14(8-6-11)22(20,21)17-15(19)16-18-9-12-3-2-4-13(12)10-18/h5-8,12-13H,2-4,9-10H2,1H3,(H2,16,17,19). InChi Key: BOVGTQGAOIONJV-UHFFFAOYSA-N.