SB-756050 is an agonist of the bile acid G protein-coupled receptor TGR5 (EC50 = 1.3 μM for the human receptor).1 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.
1.Hodge, R.J., Lin, J., Vasist Johnson, L.S., et al.Safety, pharmacokinetics, and pharmacodynamic effects of a selective TGR5 agonist, SB-756050, in type 2 diabetesClin. Pharmacol. Drug Dev.2(3)213-222(2013)