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 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.

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In DMSO USD 320 In stock
USD 170 In stock
USD 270 In stock
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Cited by 3 Publications

1 Customer Review

  • Effect of linagliptin on oxidative stress in rat hearts suffered from 9 h of hypothermic preservation followed by 60 min of reperfusion. (A) Representative image of NOX2 detected by western blotting. (B). Densitometric analysis showing the expression of NOX2 using β‑actin for normalization. Data are mean ± S.E.M. (n = 3) and expressed as fold increase relative to the value of control group. (C-E) Measurement of MnSOD activity, ROS and MDA content. Data are expressed as mean ± S.E.M., n = 8. *P < 0.05, **P < 0.01 vs control group; #P < 0.05, ##P < 0.01 vs Celsior group. NOX2: NADPH oxidase 2; MnSOD: manganese superoxide dismutase; ROS: reactive oxygen species; MDA: malondialdehyde.

    Life Sci, 2018, 210:47-54. Linagliptin purchased from Selleck.

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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.
Targets
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 MlmySpVv[3Srb36gZZN{[Xl? NVPLeGlEUW6qaXLpeIlwdiCxZjDEVHA1KGmwIHj1cYFvKEOjY3:tNkBk\WyuczDh[pRmeiBzIHjyMEBKSzVyPUGgcm0> MnfkNVg1QDV5MEO=
CHO cells MW\GeY5kfGmxbjDhd5NigQ>? MoX4SIl{eGyjY3Xt[Y51KG:oIGvOMY1mfGi7bD2zTH1{[2:yb3zhcYlv\SCocn;tJIh2dWGwIILlZ49u[mmwYX70JI12e2OjcnnubYMhVTFicnXj[ZB1d3JiZYjwdoV{e2WmIHnuJGNJVyClZXzsd{whUUN3ME2wMlI6PSEQvF2= M3:3ZlE5ODV{MEKz
HEK293 cells NEPheXBHfW6ldHnvckBie3OjeR?= NUTnZ2Z1UW6qaXLpeIlwdiCxZjDtc5V{\SC{ZXPvcYJqdmGwdDDGRXAh\XiycnXzd4VlKGmwIFjFT|I6OyClZXzsd{B2e2mwZzDBcIEuWHKxLYCtcol1em:jbnnsbYRmKGG|IIP1ZpN1emG2ZTDpcoN2[mG2ZXSg[o9zKDF3IH3pcpMheHKrb4KgeI8he3Wkc4TyZZRmKGGmZHn0bY9vNCCLQ{WwQVAvOzdizszN MkHSNlQ6ODB4OU[=
pig LLC-PK1 cells MkjlSpVv[3Srb36gZZN{[Xl? MVGxNFAh|ryP MmjTUYF5cW2jbDDpcohq[mm2aX;uJI9nKGi3bXHuJHAu\2y7Y3;wdo91\WmwIHX4dJJme3OnZDDpckBxcWdiTFzDMXBMOSClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[gX|NJZWSrZ3;4bY4he3Wkc4TyZZRmKHS{YX7zdI9zfCCjdDCxNFAhfU1iYomgcIlyfWmmIIPjbY51cWyuYYTpc44h[2:3boTpcoc> MmHwNlMxPzN5M{S=

... Click to View More Cell Line Experimental Data

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:

[1]

+ 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 Insoluble
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

* 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
NCT03869190 Not yet recruiting Urothelial Carcinoma Hoffmann-La Roche|Forty Seven Inc.Tesaro Inc. Seattle Genetics and Astellas Sanofi April 30 2019 Phase 1|Phase 2
NCT03869190 Not yet recruiting Urothelial Carcinoma Hoffmann-La Roche|Forty Seven Inc.Tesaro Inc. Seattle Genetics and Astellas Sanofi April 30 2019 Phase 1|Phase 2
NCT03629054 Completed Healthy Boehringer Ingelheim|Eli Lilly and Company August 27 2018 Phase 1
NCT03629054 Completed Healthy Boehringer Ingelheim|Eli Lilly and Company August 27 2018 Phase 1
NCT03609294 Active not recruiting Hypertension|Diabetes Boryung Pharmaceutical Co. Ltd July 18 2018 Phase 1
NCT03642184 Recruiting New Onset Diabetes After Transplant|Kidney Transplant; Complications RenJi Hospital July 14 2018 Phase 4

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