Agonist activity at human TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter gene activity incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assay
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assay
Antihyperglycemic activity in fasted ICR mouse assessed as reduction in blood glucose levels at 50 mg/kg, po measured upto 120 mins by OGTT method relative to control
Antihyperglycemic activity in overnight fasted ICR mouse assessed as reduction in blood glucose AUC (0 to 120 mins) at 50 mg/kg, po measured upto 120 mins by OGTT method relative to control
In vivo agonist activity at TGR5 in ICR mouse assessed as induction of level GLP-1 level at 50 mg/kg, po in presence of linagliptin DPP4 inhibitor by ELISA relative to control
Cmax in overnight-fasted ICR mouse systemic circulation assessed as 5-[3-(4-Cyclopropyl-3,4-dihydro-2H-quinoxaline-1-carbonyl)-pyridin-4-yloxy]-benzofuran-3-carboxylic acid at 50 mg/kg, po measured after 1 hr by LC-MS/MS analysis
Cmax in overnight-fasted ICR mouse gallbladder tissue assessed as 5-[3-(4-Cyclopropyl-3,4-dihydro-2H-quinoxaline-1-carbonyl)-pyridin-4-yloxy]-benzofuran-3-carboxylic acid at 50 mg/kg, po measured after 1 hr by LC-MS/MS analysis
Cmax in overnight-fasted ICR mouse bile assessed as 5-[3-(4-Cyclopropyl-3,4-dihydro-2H-quinoxaline-1-carbonyl)-pyridin-4-yloxy]-benzofuran-3-carboxylic acid at 50 mg/kg, po measured after 1 hr by LC-MS/MS analysis