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    InvivoChem Cat #: V0742
    CAS #: 668270-12-0Purity ≥98%

    Description: Linagliptin (formerly known as BI-1356; trade names Tradjenta and Trajenta) is a xanthine-based, highly potent, selective, and competitive DPP-4 inhibitor with potential anti-diabetic activity. It inhibits DPP-4 with an IC50 of 1 nM. DPP-4 plays a major role in the degradation of incretins such as GLP-1 which is of great importance in the process of glucose metabolism. Under physiological conditions, GLP-1 is truncated by DPP-4 rapidly, which is located on the capillary endothelium proximal to the L-cells where GLP-1 is secreted in the ileum. On 2 May 2011, Linagliptin was approved by the FDA for treatment of type II diabetes. It is being marketed by Boehringer Ingelheim and Lilly. 

    References: J Med Chem. 2007 Dec 27;50(26):6450-3; J Pharmacol Exp Ther. 2008 Apr;325(1):175-82.

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    Molecular Weight (MW)472.54
    CAS No.668270-12-0; 1198772-26-7 (Linagliptin mixture with metformin)
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 17 mg/mL (36.0 mM)
    Water:<1 mg/mL
    Ethanol: 1 mg/mL (2.1 mM)
    Solubility (In vivo)0.5% hydroxyethyl cellulose: 30 mg/mL
    SynonymsLinagliptin; BI-1356; BI1356; BI 1356; trade names: Tradjenta, Trajenta 

    Chemical Name: 8-[(3R)-3-aminopiperidin-1-yl]-7-(but-2-yn-1-yl)-3- methyl-1-[(4-methylquinazolin-2-yl)methyl]-3,7-dihydro-1H-purine-2,6-dione


    InChi Code: InChI=1S/C25H28N8O2/c1-4-5-13-32-21-22(29-24(32)31-12-8-9-17(26)14-31)30(3)25(35)33(23(21)34)15-20-27-16(2)18-10-6-7-11-19(18)28-20/h6-7,10-11,17H,8-9,12-15,26H2,1-3H3/t17-/m1/s1

    SMILES Code: O=C(N1CC2=NC(C)=C3C=CC=CC3=N2)N(C)C4=C(N(CC#CC)C(N5C[[email protected]](N)CCC5)=N4)C1=O           

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    In Vitro

    In vitro activity: Linagliptin shows a potent inhibition effect against DPP-4 in vitro and a low affinity for hERG channel and M1 receptor (IC50 295 nM). 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.

    Kinase Assay: EDTA plasma (20 μL) is diluted with 30 μL of DPP-4 assay buffer (100 mM Tris and 100 mM NaCl, adjusted to pH 7.8 with HCl) and mixed with 50 μL of H-Ala-Pro-7-amido-4-trifluoromethylcoumarin. The 200 mM stock solution in dimethylformamide is diluted 1:1000 with water to yield a final concentration of 100 μM. The plate is incubated at room temperature for 10 min, and fluorescence in the wells is determined by using a Victor 1420 Multilabel Counter at an excitation wavelength of 405 nm and an emission wavelength of 535 nm. For the detection of DPP-4 activity in wound lysates, 100 μg of protein from the respective wound lysates are used instead of 20 μL of plasma. Active GLP-1 is also detected from 100 μg of respective wound tissue samples and analyzed by using the Mouse/Rat Total Active GLP-1 Assay Kit.

    Cell Assay: A total of 4.0×107 keratinocytes per well are seeded into 24-well plates. After reaching 50% confluence, cells are starved for 24 h with DMEM. Proliferation of cells is assessed by using 1 μCi/mL of [3H]methyl-thymidine in DMEM in the presence of 10% fetal bovine serum and increasing concentrations of linagliptin (3, 30, 300, or 600 nM) for 24 h. Cells are then washed twice with phosphate-buffered saline and incubated in 5% trichloroacetic acid at 4°C for 30 min, and the DNA is solubilized in 0.5mol/LNaOH for 30 min at 37°C. Finally, [3H]thymidine incorporation is determined.

    In VivoIn 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). 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.
    Animal modelMale db/db mice
    Formulation & DosageDissolved in 0.1 N HCl and subsequently diluted with a 0.5% aqueous hydroxyethylcellulose solution (final HCl concentration 3 mM); 1 mg/kg; p.o. administration
    ReferencesJ Med Chem. 2007 Dec 27;50(26):6450-3; J Pharmacol Exp Ther. 2008 Apr;325(1):175-82.

    These protocols are for reference only. InvivoChem does not independently validate these methods.



    Chemical structures (A) and in vitro potency (B) of BI 1356 and other DPP-4 inhibitors. J Pharmacol Exp Ther. 2008 Apr;325(1):175-82. 


    Dissociation of BI 1356 and vildagliptin from the DPP-4 enzyme. J Pharmacol Exp Ther. 2008 Apr;325(1):175-82. 


    Inhibition of DPP-4 activity ex vivo in plasma obtained from HanWistar rats after single oral administration of BI 1356 at different doses. J Pharmacol Exp Ther. 2008 Apr;325(1):175-82. 


    Inhibition of plasma DPP-4 activity in HanWistar rats after single oral dosing of various inhibitors. J Pharmacol Exp Ther. 2008 Apr;325(1):175-82. 


    OGTT in C57BL/6J mice after oral administration of various DPP-4 inhibitors at doses of 1 or 10 mg/kg (A–C). J Pharmacol Exp Ther. 2008 Apr;325(1):175-82. 


    OGTT in Zucker fatty rats cannulated in the right carotid artery for blood sampling. J Pharmacol Exp Ther. 2008 Apr;325(1):175-82. 


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