Catalog No.S3031 Synonyms: BI-1356
Molecular Weight(MW): 472.54
Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM.
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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
|Description||Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM.|
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 vivo||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)|
|Ethanol||1 mg/mL (2.11 mM)|
|In vivo||0.5% hydroxyethyl cellulose||30 mg/mL|
* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02768220||Not yet recruiting||SGLT-2 Inhibitors|Advanced Glycation End Products|Diabetes||Northwell Health||July 2017||Phase 4|
|NCT03051243||Not yet recruiting||DM2||Rabin Medical Center||February 2017||Phase 3|
|NCT03011177||Not yet recruiting||Type2 Diabetes Mellitus||Handok Pharmaceuticals Co., Ltd.||January 2017||Phase 4|
|NCT02897349||Recruiting||Diabetes Mellitus, Type 2||Boehringer Ingelheim|Eli Lilly and Company||September 2016||Phase 3|
|NCT02974504||Recruiting||Type2 Diabetes||Dong-A ST Co., Ltd.||September 2016||Phase 4|
|NCT02815644||Completed||Healthy||Boehringer Ingelheim||July 2016||Phase 1|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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