A sulfonylurea and an inhibitor of pancreatic β-cell KATP channels (IC50 = 184 nM for murine β-cells); selective for pancreatic β-cell over cardiac and arterial smooth muscle cell KATP channels (IC50s = 19.5 and 37.9 μM

Gliclazide – 5 g

Brand:
Cayman
CAS:
21187-98-4
Storage:
4
UN-No:
Non-Hazardous - /

Gliclazide is a sulfonylurea and an inhibitor of pancreatic β-cell ATP-sensitive potassium (KATP) channels (IC50 = 184 nM for murine β-cells).{47058,34125} It is selective for pancreatic β-cell over cardiac and arterial smooth muscle cell KATP channels (IC50s = 19.5 and 37.9 μM, respectively).{47058} 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.{47059} Gliclazide (5 and 10 μg/ml) reduces LDL oxidation by human aortic smooth muscle cells (HASMCs), decreasing TBARS content and 8-isoprostane levels.{8975} It also decreases oxidized LDL-induced HASMC proliferation and monocyte adhesion when used at concentrations ranging from 1 to 10 μg/ml. Gliclazide (5mg/kg) reduces serum glucose levels and increases glucose uptake by isolated rat hindquarters in a model of diabetes induced by streptozotocin (STZ; Item No. 13104).{47060}  

 

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Description

A sulfonylurea and an inhibitor of pancreatic β-cell KATP channels (IC50 = 184 nM for murine β-cells); selective for pancreatic β-cell over cardiac and arterial smooth muscle cell KATP channels (IC50s = 19.5 and 37.9 μM, respectively); increases insulin-induced glucose uptake and GLUT4 translocation to the plasma membrane in a differentiated 3T3L1 adipocyte model of insulin resistance induced by hydrogen peroxide at 5 μM; reduces LDL oxidation by HASMCs, decreasing TBARS content and 8-isoprostane levels at 5 and 10 μg/ml; decreases oxidized LDL-induced HASMC proliferation and monocyte adhesion at 1-10 μg/ml; reduces serum glucose levels and increases glucose uptake by isolated rat hindquarters in a model of diabetes induced by STZ at 5mg/kg

Formal name: N-[[(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)amino]carbonyl]-4-methyl-benzenesulfonamide

Synonyms: 

Molecular weight: 323.4

CAS: 21187-98-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Product Type|Biochemicals|Ox Stress Reagents|Antioxidants||Research Area|Cardiovascular System|Cardiovascular Diseases|Atherosclerosis||Research Area|Cardiovascular System|Lipids & Lipoproteins|Lipoproteins||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes||Research Area|Oxidative Stress & Reactive Species|Antioxidant Activity||Research Area|Oxidative Stress & Reactive Species|Lipid Peroxidation

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