TAK-875 is an orally-available, benzofuran-based, agonist of GPR40 for the potential treament of Type 2 diabetes mellitus, with an human EC50 of 0.014 uM in a FLIPR assay. It has high selectivity over GPR41, GPR43, and GPR120, with EC50s all greater than 10 uM. [1] Oral dosing (0.3-3 mg/kg) of TAK-875 in a glucose intolerance test in female Wistar rats reduced blood glucose excursion. Insulin secretion was increased during an oral glucose tolerance test.

TAK-875 was shown to activate the Gqa-mediated signalling pathway in pancreatic b-cells. Prolonged agonist stimulation by TAK-875 revealed no evidence of b-cell dysfunction or toxicity, nor does it cause a induction of a marker of apoptosis in pancreatic b-cells. [2]

TAK-875 is an orally-available, benzofuran-based, agonist of GPR40 for the potential treament of Type 2 diabetes mellitus, with an human EC50 of 0.014 uM in a FLIPR assay. It has high selectivity over GPR41, GPR43, and GPR120, with EC50s all greater than 10 uM. [1] Oral dosing (0.3-3 mg/kg) of TAK-875 in a glucose intolerance test in female Wistar rats reduced blood glucose excursion. Insulin secretion was increased during an oral glucose tolerance test.

TAK-875 was shown to activate the Gqa-mediated signalling pathway in pancreatic b-cells. Prolonged agonist stimulation by TAK-875 revealed no evidence of b-cell dysfunction or toxicity, nor does it cause a induction of a marker of apoptosis in pancreatic b-cells. [2]