TGR5 agonist MN6 is a potent and selective TGR5 agonist with cAMP EC50 values of 15.9 nM and 17.9 nM on hTGR5 and mTGR5, respectively.
MN6 shows EC50 values of 1.5 and 18 nM on hTGR5 and mTGR5, respectively, by a CRE-driven luciferase reporter gene assay in either the hTGR5/CRE/HEK293 or mTGR5/CRE/HEK293 stable cell line.
MN6 significantly promoted GLP-1 secretion in human enteroendocrine NCI-H716 cells in a dose-dependent manner.
MN6 increased the plasma active GLP-1 level in CD1 mice following a glucose bolus, with a 68.5% or 89.3% increase after a single dose of 50 or 100 mg/kg MN6, respectively.
MN6 exhibited a synergistic effect combined with DPP-4 inhibitor BI-1356 (Cat. PC-42508).
MN6 (50 mg/kg) improved glucose homeostasis in ob/ob mice, improved metabolic abnormalities and increased the insulinstimulated glucose uptake in the skeletal muscles of DIO mice.
