Linagliptin 668270-12-0

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Molecular Weight:

472.54 Linagliptin is a highly potent, selective DPP-4 Inhibitor with IC50 of 1 nM.






Biological Activity


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.


In male Wistar rats, Beagle dogs, and Rhesus monkeys, Linagliptin shows a
highly efficacious, long-lasting, and potent inhibitory activity
against DPP-4 by more than 70% inhibition for all three species after
oral administration of 1 mg/kg. Oral administration of Linagliptin to
db/db mice 45 min before an oral glucose tolerance test reduces plasma
glucose excursion in a dose-dependent manner from 0.1 mg/kg (15%
inhibition) to 1 mg/kg (66% inhibition).


By inhibiting
DPP-4 activity, Linagliptin reduces the expression of the
proinflammatory markers cyclooxygenase-2 and macrophage inflammatory
protein-2, and enhances the formation of myofibroblasts in healing
wounds from ob/ob mice.

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Product Categories : Proteases > DPP-4 Inhibitor