Linagliptin

Catalog No.S3031

Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM.

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Linagliptin Chemical Structure

Linagliptin Chemical Structure
Molecular Weight: 472.54

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

Linagliptin is available in the following compound libraries:

Product Information

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Product Description

Biological Activity

Description Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM.
Targets DPP-4 [1]
IC50 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]
Features

Protocol(Only for Reference)

Kinase Assay:

[1]

In Vitro DPP-4 Inhibition Assay For determination of the in vitro potency of inhibitors, an extract from the human colon carcinoma cell line Caco-2 is used as source of the DPP-4 enzyme. Caco-2 cells are grown to confluency in cell culture flasks in EMEM medium supplemented with non-essential amino acids and containing 10% heat-inactivated fetal calf serum. Cells are washed with PBS and 4 mL lysis buffer (10 mM Tris-HCl, 150 mM NaCl, 0.04 U/mL aprotinin, 0.5% Nonidet P40, pH 8.0) are added per flask. After 5 minute incubation at room temperature with gentle agitation, cells are centrifuged at 4 °C for 30 minutes and the supernatant is stored at -80°C. Prior to use, the extract is diluted 1000-fold with assay buffer (100 mM Tris-HCl, 100 mM NaCl, pH 7.8).

Animal Study:

[1]

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Eckhardt M, et al. J Med Chem. 2007, 50(26), 6450-6453.

[2] Thomas L, J Pharmacol Exp Ther. 2008, 325(1), 175-182.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02768220 Not yet recruiting SGLT-2 Inhibitors|Advanced Glycation End Products|Diabetes Northwell Health August 2016 Phase 4
NCT02821910 Not yet recruiting Healthy Boehringer Ingelheim|Eli Lilly and Company July 2016 Phase 1
NCT02815644 Not yet recruiting Healthy Boehringer Ingelheim July 2016 Phase 1
NCT02792400 Enrolling by invitation Type 2 Diabetes University Hospital, Gentofte, Copenhagen|Eli Lilly and C  ...more University Hospital, Gentofte, Copenhagen|Eli Lilly and Company May 2016 --
NCT02758171 Active, not recruiting Healthy Boehringer Ingelheim|Eli Lilly and Company May 2016 Phase 1

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Chemical Information

Download Linagliptin SDF
Molecular Weight (MW) 472.54
Formula

C25H28N8O2

CAS No. 668270-12-0
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms BI-1356
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 Name (R)-8-(3-aminopiperidin-1-yl)-7-(but-2-ynyl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-1H-purine-2,6(3H,7H)-dione

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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