Linagliptin (BI-1356)

Catalog No.S3031 Synonyms: GSK2118436

For research use only.

Linagliptin (BI-1356,GSK2118436) 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 (BI-1356) Chemical Structure

CAS No. 668270-12-0

Selleck's Linagliptin (BI-1356) has been cited by 14 publications

Purity & Quality Control

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Biological Activity

Description Linagliptin (BI-1356,GSK2118436) 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.
Targets
Ferroptosis [4] DPP-4 [1]
(cell-free assay)
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human Caco-2 cells M4HqNGZ2dmO2aX;uJIF{e2G7 M3O4U2lvcGmkaYTpc44hd2ZiRGDQOEBqdiCqdX3hckBE[WOxLUKgZ4VtdHNiYX\0[ZIhOSCqcjygTWM2OD1zIH7N MW[xPFQ5PTdyMx?=
CHO cells M3PtVWZ2dmO2aX;uJIF{e2G7 MnXpSIl{eGyjY3Xt[Y51KG:oIGvOMY1mfGi7bD2zTH1{[2:yb3zhcYlv\SCocn;tJIh2dWGwIILlZ49u[mmwYX70JI12e2OjcnnubYMhVTFicnXj[ZB1d3JiZYjwdoV{e2WmIHnuJGNJVyClZXzsd{whUUN3ME2wMlI6PSEQvF2= NUnYeGFNOThyNUKwNlM>
HEK293 cells NUfEboF7TnWwY4Tpc44h[XO|YYm= NYDD[INQUW6qaXLpeIlwdiCxZjDtc5V{\SC{ZXPvcYJqdmGwdDDGRXAh\XiycnXzd4VlKGmwIFjFT|I6OyClZXzsd{B2e2mwZzDBcIEuWHKxLYCtcol1em:jbnnsbYRmKGG|IIP1ZpN1emG2ZTDpcoN2[mG2ZXSg[o9zKDF3IH3pcpMheHKrb4KgeI8he3Wkc4TyZZRmKGGmZHn0bY9vNCCLQ{WwQVAvOzdizszN MoLpNlQ6ODB4OU[=
pig LLC-PK1 cells M1rmemZ2dmO2aX;uJIF{e2G7 MoXtNVAxKM7:TR?= M{P6O21igGmvYXygbY5pcWKrdHnvckBw\iCqdX3hckBRNWeueXPvdJJwfGWrbjDlfJBz\XO|ZXSgbY4heGmpIFzMR{1RUzFiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIH;mJHs{UF2maXfvfIlvKHO3YoP0doF1\SC2cnHud5BwenRiYYSgNVAxKHWPIHL5JIxqeXWrZDDzZ4lvfGmubHH0bY9vKGOxdX70bY5o NFfycIUzOzB5M{ezOC=>
Assay
Methods Test Index PMID
Western blot Cyclin D1 / p27 28177527
Growth inhibition assay Cell viability ; Cell viability 28177527 26010513
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 (from reference)

Animal Research:

[1]

  • Animal Models: Male db/db mice
  • Dosages: ≤1 mg/kg
  • Administration: Administered via p.o.

Solubility (25°C)

In vitro

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.

30 mg/mL

Chemical Information

Molecular Weight 472.54
Formula

C25H28N8O2

CAS No. 668270-12-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC#CCN1C2=C(N=C1N3CCCC(C3)N)N(C(=O)N(C2=O)CC4=NC5=CC=CC=C5C(=N4)C)C

In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04180813 Terminated 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

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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.

Handling Instructions

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