447410-57-3

SB-756050 is an agonist of the bile acid G protein-coupled receptor TGR5 (EC₅₀ = 1.3 μM for the human receptor). It is selective for TGR5 over the farnesoid X receptor (FXR) and a panel of other receptors, channels, and transporters. SB-756050 (10-100 mg/kg) decreases fasting glucose levels and increases glucose disposal rate and insulin secretion in diabetic Goto Kakizaki rats.