Cayman Pf-00835231

Gliclazide-d₄ is intended for use as an internal standard for the quantification of gliclazide (Item No. ) by GC- or LC-MS. Gliclazide is a sulfonylurea and an inhibitor of pancreatic β-cell ATP-sensitive potassium (K_ATP) channels (IC₅₀ = 184 nM for murine β-cells).^, It is selective for pancreatic β-cell over cardiac and arterial smooth muscle cell K_ATP 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; Item No. ).

WARNING This product is not for human or veterinary use.