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.

Size Price Stock Quantity  
In DMSO USD 320 In stock
USD 170 In stock
USD 270 In stock
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Cited by 4 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.

Purity & Quality Control

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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 M4TaSGZ2dmO2aX;uJIF{e2G7 NIe0VpJKdmirYnn0bY9vKG:oIFTQVFQhcW5iaIXtZY4hS2Glbz2yJINmdGy|IHHmeIVzKDFiaIKsJGlEPTB;MTDuUS=> MnPQNVg1QDV5MEO=
CHO cells NIGxVlRHfW6ldHnvckBie3OjeR?= MVXEbZNxdGGlZX3lcpQhd2ZiW16tcYV1cHmuLUPIYZNkd3CxbHHtbY5mKG[{b32gbJVu[W5icnXjc41jcW6jboSgcZV{[2G{aX7pZ{BOOSC{ZXPldJRweiCneIDy[ZN{\WRiaX6gR2hQKGOnbHzzMEBKSzVyPUCuNlk2KM7:TR?= NETTTpkyQDB3MkCyNy=>
HEK293 cells M2WxVWZ2dmO2aX;uJIF{e2G7 NX36ZWNrUW6qaXLpeIlwdiCxZjDtc5V{\SC{ZXPvcYJqdmGwdDDGRXAh\XiycnXzd4VlKGmwIFjFT|I6OyClZXzsd{B2e2mwZzDBcIEuWHKxLYCtcol1em:jbnnsbYRmKGG|IIP1ZpN1emG2ZTDpcoN2[mG2ZXSg[o9zKDF3IH3pcpMheHKrb4KgeI8he3Wkc4TyZZRmKGGmZHn0bY9vNCCLQ{WwQVAvOzdizszN NGK5R40zPDlyME[5Oi=>
pig LLC-PK1 cells MoHJSpVv[3Srb36gZZN{[Xl? MVWxNFAh|ryP MWPNZZhqdWGuIHnubIljcXSrb36gc4YhcHWvYX6gVE1odHmlb4Dyc5RmcW5iZYjwdoV{e2WmIHnuJJBq\yCOTFOtVGsyKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCxZjDbN2he\Gmpb4jpckB{fWK|dILheIUhfHKjboPwc5J1KGG2IEGwNEB2VSCkeTDsbZF2cWRic3PpcpRqdGyjdHnvckBkd3WwdHnu[y=> M2SyVFI{ODd|N{O0

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Cyclin D1 / p27 ; 

PubMed: 28177527     


Effects of linagliptin on the expression of cyclin D1 and p27 in immortalized human podocytes. Immortalized human podocytes were exposed to either vehicle alone (control) or linagliptin (100 nM) for 5 days, then the expression of cyclin D1 and p27 was evaluated by western blot analyses. β‐Actin was adopted as an internal standard to control for unwanted sources of variation. Each image is representative of five experiments run in duplicate for each experimental group.

28177527
Growth inhibition assay
Cell viability ; 

PubMed: 28177527     


Immortalized human podocytes were exposed to vehicle alone (control) or increasing concentrations of either linagliptin (0.01–100 nM; 5 days) or sitagliptin (0.01–1000 nM; 5 days), and cell growth was measured as described above. To set the Y axis, all data were normalized to the mean value of the control group (0%). Data are expressed as mean ± SEM of six experiments run in triplicate for each experimental group. *P < 0.05 versus control group.

Cell viability; 

PubMed: 26010513     


Dose effects of linagliptin on SK-N-MC cells by MTT assay. Linagliptin shows no significant cytotoxicity

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

Animal Research:

[1]

- Collapse
  • 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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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