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CAS No. 668270-12-0
Linagliptin (BI-1356) is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM and exhibits a 10,000-fold higher selectivity for DPP-4 than for other dipeptidyl peptidases such as DPP-2, DPP-8, and DPP-9. Linagliptin activates glomerular autophagy in a model of type 2 diabetes. DPP4 mediates ferroptosis in TP53-deficient CRC cells.
Selleck's Linagliptin (BI-1356) has been cited by 8 publications
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Effect of linagliptin on oxidative stress in rat hearts suffered from 9 h of hypothermic preservation followed by 60 min of reperfusion. (A) Representative image of NOX2 detected by western blotting. (B). Densitometric analysis showing the expression of NOX2 using β‑actin for normalization. Data are mean ± S.E.M. (n = 3) and expressed as fold increase relative to the value of control group. (C-E) Measurement of MnSOD activity, ROS and MDA content. Data are expressed as mean ± S.E.M., n = 8. *P < 0.05, **P < 0.01 vs control group; #P < 0.05, ##P < 0.01 vs Celsior group. NOX2: NADPH oxidase 2; MnSOD: manganese superoxide dismutase; ROS: reactive oxygen species; MDA: malondialdehyde.
Life Sci, 2018, 210:47-54. Linagliptin (BI-1356) purchased from Selleck.
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Choose Selective DPP-4 Inhibitors
|Description||Linagliptin (BI-1356) is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM and exhibits a 10,000-fold higher selectivity for DPP-4 than for other dipeptidyl peptidases such as DPP-2, DPP-8, and DPP-9. Linagliptin activates glomerular autophagy in a model of type 2 diabetes. DPP4 mediates ferroptosis in TP53-deficient CRC cells.|
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. 
|In vitro||DMSO||17 mg/mL (35.97 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
0.5% hydroxyethyl cellulose
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04180813||Recruiting||Drug: Linagliptin|Drug: Acarbose||Diabetes Mellitus Type 2||Boehringer Ingelheim||March 4 2020||--|
|NCT02815644||Completed||Drug: empagliflozin/linagliptin FDC||Healthy||Boehringer Ingelheim||July 15 2016||Phase 1|
|NCT02758171||Completed||Drug: Empagliflozin|Drug: Linagliptin||Healthy||Boehringer Ingelheim|Eli Lilly and Company||May 17 2016||Phase 1|
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