Linagliptin

CAS No : 668270-12-0

Molecular Weight: 472.54

Synonym(s):

(R)-8-(3-Amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione, 8-(3-(R)-Aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione, BI 1356, BI-1356, BI1356, Ondero

Empirical Formula : C₂₅H₂₈N₈O₂

Description :

Linagliptin is an orally active, competitive, potent and selective dipeptidyl peptidase IV (DPP4; DPP-IV) inhibitor (IC50 = 1 nM vs. 19 nM/sitagliptin, 24 nM/alogliptin, 50 nM/saxagliptin, 62 nM/vildagliptin) with no inhibitory potency against DPP-2/8/9 (IC50 >10 µM). Sitagliptin improves glucose tolerance and exhibits efficacy in diabetic rodent models in vivo (1-10 mg/kg via daily p.o. in mice and rats).