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 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.

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

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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.

Biological Activity

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.
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]


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


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 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

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DPP-4 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID