格列喹酮
Gliquidone (Synonyms: AR-DF 26)
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基本信息
中文名称格列喹酮
英文名称 Gliquidone (Synonyms: AR-DF 26)
CAS号33342-05-1
分子式C27H33N3O6S
分子量527.63
外观White crystalline powder, odorless
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Gliquidone (Glurenorm,AR-DF 26) is an ATP-sensitive K+ channel antagonist with IC50 of 27.2 nM.

Gliquidone is a second generation sulfonylurea that selectively inhibits ATP-sensitive potassium channel currents (IKATP) in pancreatic β-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 γ (PPARγ) 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; Item No. 13104) when administered at a dose of 10 mg/kg.

Gliquidone (AR-DF 26) is an anti-diabetic agent in the sulfonylurea class, used in the treatment of diabetes mellitus type 2.


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格列喹酮