Home Proteases DPP inhibitor - Ferroptosis inhibitor - Autophagy activator Linagliptin (GSK2118436) For research use only.

Linagliptin (GSK2118436)

Synonyms: BI-1356

Linagliptin (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 (GSK2118436) Chemical Structure

Linagliptin (GSK2118436) Chemical Structure

CAS No. 668270-12-0

Purity & Quality Control

Linagliptin (GSK2118436) Related Products

Signaling Pathway

DPP Signaling Pathways

DPP Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human Caco-2 cells Function assay Inhibition of DPP4 in human Caco-2 cells after 1 hr, IC50=1 nM 18485703
CHO cells Function assay Displacement of [N-methyl-3H]scopolamine from human recombinant muscarinic M1 receptor expressed in CHO cells, IC50=0.295 μM 18052023
HEK293 cells Function assay Inhibition of mouse recombinant FAP expressed in HEK293 cells using Ala-Pro-p-nitroanilide as substrate incubated for 15 mins prior to substrate addition, IC50=0.37 μM 24900696
pig LLC-PK1 cells Function assay 100 μM Maximal inhibition of human P-glycoprotein expressed in pig LLC-PK1 cells assessed as reduction of [3H]digoxin substrate transport at 100 uM by liquid scintillation counting 23073734
Click to View More Cell Line Experimental Data

Biological Activity

Description Linagliptin (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
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]
Experimental Result Images Methods Biomarkers Images PMID
Western blot Cyclin D1 / p27 28177527
Growth inhibition assay Cell viability Cell viability 28177527
In Vivo
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 Animal Models Male db/db mice
Dosages ≤1 mg/kg
Administration Administered via p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04180813 Terminated
Diabetes Mellitus Type 2
Boehringer Ingelheim
 March 4 2020 --

Chemical Information & Solubility

Molecular Weight 472.54 Formula

C25H28N8O2
CAS No. 668270-12-0 SDF Download Linagliptin (GSK2118436) SDF
Smiles CC#CCN1C2=C(N=C1N3CCCC(C3)N)N(C(=O)N(C2=O)CC4=NC5=CC=CC=C5C(=N4)C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 17 mg/mL ( (35.97 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 1 mg/mL

Water : Insoluble


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In vivo
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