DC260126 | GPR40 antagonist

DC260126 (346692-04-4) is a GPR40 receptor antagonist¹. Suppresses fatty acid-induced elevation of intracellular Ca⁺⁺. Inhibits palmitic acid potentiated glucoseÐstimulated insulin secretion in Min6 pancreatic β cells in vitro. DC260126 lowers serum insulin levels, increases insulin sensitivity² in obese Zucker rats (6 mg/kg)². Reduces pancreatic β cell apoptosis in obese diabetic (db/db) rats³. Protects Min6 β cells from palmitic acid-induced ER stress and apoptosis⁴

References/Citations
1) Hu et al. (2009), A novel class of antagonist for the FFAs receptor GPR40; Biochem. Biophys. Res. Commun., 390 557
2) Zhang et al. (2010), DC260126, a small molecule antagonist of GPR40, improves insulin tolerance but not glucose tolerance in obese Zucker rats; Biomed. Pharmacother., 64 647
3) Sun et al. (2013), DC260126: a small molecule antagonist of GPR40 that protects against pancreatic β-cells dysfunction in db/db mice; PLoS One., 8(6) e66744
4) Wu et al. (2012), Inhibition of GPR40 protects MIN6 β cells from palmitate-induced ER stress and apoptosis; J. Biochem, 113 1152