BI-1356 (Linagliptin) is a highly potent and selective dipeptidyl peptidase 4 (DPP-4) inhibitor (IC50 = 1 nM) for treatment of type II diabetes. [1] BI-1356 can increase incretin levels (GLP-1 and GIP), which increases insulin secretion and inhibits glucagon release, decreases gastric emptying, and decreases blood glucose levels. BI-1356 shows 10,000-fold more selectivity for DPP-4 against other protease/peptidases, including DPP-8, DPP-9, trypsin, plasmin, and thrombin.[2]

BI-1356 (Linagliptin) is a highly potent and selective dipeptidyl peptidase 4 (DPP-4) inhibitor (IC50 = 1 nM) for treatment of type II diabetes. [1] BI-1356 can increase incretin levels (GLP-1 and GIP), which increases insulin secretion and inhibits glucagon release, decreases gastric emptying, and decreases blood glucose levels. BI-1356 shows 10,000-fold more selectivity for DPP-4 against other protease/peptidases, including DPP-8, DPP-9, trypsin, plasmin, and thrombin.[2]