Linagliptin

Catalog No.S3031 Synonyms: BI-1356

Linagliptin Chemical Structure

Molecular Weight(MW): 472.54

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

Size Price Stock Quantity  
In DMSO USD 320 In stock
USD 170 In stock
USD 270 In stock

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Notes:

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.

Biological Activity

Description Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM.
Targets
DPP-4 [1]
1 nM
In vitro

Linagliptin shows a potent inhibition effect against DPP-4 in vitro and a low affinity for hERG channel and M1 receptor (IC50 295 nM). [1] 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. [2]

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). [1] 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. [3]

Protocol

Animal Research
+ Expand
  • Animal Models: Male db/db mice
  • Formulation: Linagliptin is dissolved in 0.1 N HCl and subsequently diluted with a 0.5% aqueous hydroxyethylcellulose solution (final HCl concentration 3 mM).
  • Dosages: ≤1 mg/kg
  • Administration: Administered via p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 17 mg/mL (35.97 mM)
Ethanol 1 mg/mL (2.11 mM)
Water <1 mg/mL
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.

Chemical Information

Molecular Weight 472.54
Formula

C25H28N8O2

CAS No. 668270-12-0
Storage powder
in solvent
Synonyms BI-1356

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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 August 2016 Phase 4
NCT02821910 Not yet recruiting Healthy Boehringer Ingelheim|Eli Lilly and Company July 2016 Phase 1
NCT02815644 Not yet recruiting Healthy Boehringer Ingelheim July 2016 Phase 1
NCT02792400 Enrolling by invitation Type 2 Diabetes University Hospital, Gentofte, Copenhagen|Eli Lilly and Company May 2016 --
NCT02758171 Active, not recruiting Healthy Boehringer Ingelheim|Eli Lilly and Company May 2016 Phase 1
NCT02752113 Recruiting Diabetes Mellitus Type 2 Institut für Pharmakologie und Präventive Medizin|University of Erlangen-Nürnberg Medical School April 2016 Phase 3

Tech Support

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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DPP-4 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID