Linagliptin shows a potent inhibition effect against DPP-4 in vitro and a low affinity for hERG channel and M1 receptor (IC50 295 nM). Linagliptin acts as a competitive inhibitor with a Ki of 1 nM, and also shows 10,000-fold more selectivity for DPP-4 than DPP-8, DPP-9, amino-peptidases N and P, prolyloligopeptidase, trypsin, plasmin, and thrombin, and 90-fold more selectivity than fibroblast activation protein in vitro.

June 21, 2017

prudect name : Linagliptin shows a potent inhibition effect against DPP-4 in vitro and a low affinity for hERG channel and M1 receptor (IC50 295 nM). Linagliptin acts as a competitive inhibitor with a Ki of 1 nM, and also shows 10,000-fold more selectivity for DPP-4 than DPP-8, DPP-9, amino-peptidases N and P, prolyloligopeptidase, trypsin, plasmin, and thrombin, and 90-fold more selectivity than fibroblast activation protein in vitro.
Linagliptin (BI-1356)

Synonyms: CAS NO: 668270-12-0Molecular Formula: C₂₅H₂₈N₈O₂Molecular Weight: 472.54Purity: 98% minSolubility: In DMSOStorage: -20°C

web site: www.medchemexpress.com

References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18524965