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 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.
Purity & Quality Control
Choose Selective DPP-4 Inhibitors
|Description||Linagliptin 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 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||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
0.5% hydroxyethyl cellulose
For best results, use promptly after mixing.
* 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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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03259490||Completed||Healthy||Boehringer Ingelheim|Eli Lilly and Company||August 31 2017||Phase 1|
|NCT02897349||Recruiting||Diabetes Mellitus Type 2||Boehringer Ingelheim|Eli Lilly and Company||September 30 2016||Phase 3|
|NCT03320031||Recruiting||Type 2 Diabetes Mellitus|Peritoneal Dialysis||Yanbing Li|Sun Yat-sen University||June 3 2017||Phase 4|
|NCT03629054||Recruiting||Healthy||Boehringer Ingelheim|Eli Lilly and Company||August 27 2018||Phase 1|
|NCT01243424||Completed||Diabetes Mellitus Type 2||Boehringer Ingelheim|Eli Lilly and Company||October 26 2010||Phase 3|
|NCT02061969||Completed||Diabetes||Emory University|American Diabetes Association||April 25 2014||Phase 4|
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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