A second generation sulfonylurea; selectively inhibits IKATP in pancreatic β-cells (IC50s = 0.45

Gliquidone – 1 g

Brand:
Cayman
CAS:
33342-05-1
Storage:
-20
UN-No:
Non-Hazardous - /

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).{49421} It is also a peroxisome proliferator-activated receptor γ (PPARγ) agonist (EC50 = 10 μM in a transactivation assay).{49422} Gliquidone (0.2 nmol/g) decreases plasma levels of D-glucose and stimulates insulin release in anesthetized rats.{49423} 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.{49424}  

 

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SKU: 29596 - 1 g Category:

Description

A second generation sulfonylurea; selectively inhibits 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); PPARγ agonist (EC50 = 10 μM in a transactivation assay); decreases plasma levels of D-glucose and stimulates insulin release in anesthetized rats at 0.2 nmol/g; decreases blood glucose levels, serum ALP, AST, and ALT activities, and hepatic lipid peroxidation and increases hepatic GSH levels in a rat model of STZ-induced at 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

Synonyms:  AR-DF 26

Molecular weight: 527.6

CAS: 33342-05-1

Purity: ≥98%

Formulation: A crystalline solid

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