Agonist activity at human FXR expressed in human Huh-7 cells co-transfected with FXRE-Luc reporter plasmid assessed as receptor transactivation incubated for 16 hrs by luciferase reporter gene assay
Agonist activity at human FXR expressed in human Huh-7 cells co-transfected with FXRE-Luc reporter plasmid assessed as receptor transactivation incubated for 16 hrs by luciferase reporter gene assay relative to OCA
Agonist activity at human TGR5 expressed in HEK293 cells co-transfected with CRE-Luc reporter plasmid assessed as receptor transactivation incubated for 5.5 hrs by luciferase reporter gene assay
Agonist activity at human TGR5 expressed in HEK293 cells co-transfected with CRE-Luc reporter plasmid assessed as receptor transactivation incubated for 5.5 hrs by luciferase reporter gene assay relative to OCA
Agonist activity at FXR in C57BL/6J mouse hepatocytes assessed as fold upregulation of SHP mRNA expression at 10 uM incubated for 24 hrs by qRT-PCR analysis relative to control
Agonist activity at FXR in C57BL/6J mouse hepatocytes assessed as upregulation of BSEP mRNA expression at 0.4 to 10 uM incubated for 24 hrs by qRT-PCR analysis
In vivo agonist activity at FXR in C57BL/6J mouse assessed as fold upregulation of SHP mRNA expression in liver at 10 mg/kg, po measured after 6 hrs by qRT-PCR analysis relative to control
In vivo agonist activity at FXR in C57BL/6J mouse assessed as downregulation of CYP7A1 mRNA expression in liver at 10 mg/kg, po measured after 6 hrs by qRT-PCR analysis
In vivo agonist activity at FXR in C57BL/6J mouse assessed as downregulation of CYP8B1 mRNA expression in liver at 10 mg/kg, po measured after 6 hrs by qRT-PCR analysis
In vivo agonist activity at FXR in C57BL/6J mouse assessed as fold upregulation of SHP mRNA expression in ileum at 10 mg/kg, po measured after 6 hrs by qRT-PCR analysis relative to control
In vivo agonist activity at FXR in C57BL/6J mouse assessed as fold upregulation of FGF15 mRNA expression in ileum at 10 mg/kg, po measured after 6 hrs by qRT-PCR analysis relative to control