Linagliptin is a highly potent, selective CD26 (DPP-4) inhibitor with IC50 of 1 nM. Linagliptin was observed to be 10,000-fold more selective for DPP-4 over 11 other peptidases and proteases studied in a test. Linagliptin can also inhibit up to 90% of DPP-4 activity in rat plasma. In Zucker diabetic fatty rats, Linagliptin can dose-dependently decrease plasma glucose and increase plasma levels of glucagon-like peptide 1 and insulin. When administered orally, Linagliptin reduced HbA1c levels in mice with high-fat diets and low-dose streptozotocin-induced diabetes. Type 2 diabetes mellitus has been treated using formulations containing Linagliptin.
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