1. Metabolic Enzyme/Protease
    Autophagy
    Apoptosis
  2. Dipeptidyl Peptidase
    Autophagy
    Ferroptosis
  3. Linagliptin

Linagliptin (Synonyms: BI 1356)

Cat. No.: HY-10284 Purity: 99.97%
Handling Instructions

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

For research use only. We do not sell to patients.

Linagliptin Chemical Structure

Linagliptin Chemical Structure

CAS No. : 668270-12-0

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Solution
10 mM * 1 mL in DMSO USD 61 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
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Estimated Time of Arrival: December 31
Solid
100 mg USD 66 In-stock
Estimated Time of Arrival: December 31
500 mg USD 99 In-stock
Estimated Time of Arrival: December 31
1 g USD 176 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 7 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Linagliptin purchased from MCE. Usage Cited in: Sci Rep. 2017 Jun 28;7(1):4351.

    Western blot analysis of CREB protein phosphorylation in pancreas of KKAy mice treated with HBK001 and Linagliptin.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

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

    IC50 & Target

    IC50: 1 nM (DPP-4)

    In Vitro

    Linagliptin inhibits DPP-4 activity in vitro in several independent experiments with IC50 values of 0.4, 0.5, 0.9, and 1.1 nM (mean IC50, approximately 1 nM). Linagliptin inhibits FAP with an IC50 of 89 nM (approximately 90-fold selectivity versus DPP-4)[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    In male Wistar rats, Beagle dogs, and Rhesus monkeys, xanthine linagliptin proves to be a highly efficacious, long-lasting, and potent DPP-4 inhibitor providing >70% inhibition for >7 h for all three species after oral administration of 1 mg/kg. Single oral administration of linagliptin to db/db mice 45 min prior to an oral glucose tolerance test reduced plasma glucose excursion in a dose-dependent manner from 0.1 mg/kg (15% inhibition) to 1 mg/kg (66% inhibition)[1]. Linagliptin (3 and 10 mg/kg) dose-dependently inhibits the DPP-4 enzyme in plasma within 30 min of administration. Linagliptin (1 mg/kg, p.o.) significantly reduces glucose excursion by approximately 50%[2]. Oral administration of the DPP-4 inhibitor linagliptin (3 mg/kg, p.o.) strongly reduces DPP-4 activity, stabilizes active GLP-1 in chronic wounds, and improves healing in ob/ob mice. At day 10 postwounding, linagliptin-treated ob/ob mice show largely epithelialized wounds characterized by the absence of neutrophils[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    Molecular Weight

    472.54

    Formula

    C25H28N8O2

    CAS No.
    SMILES

    O=C1N(C2=C(C(N1CC3=NC(C)=C4C=CC=CC4=N3)=O)N(CC#CC)C(N5CCC[[email protected]@H](N)C5)=N2)C

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (105.81 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1162 mL 10.5811 mL 21.1622 mL
    5 mM 0.4232 mL 2.1162 mL 4.2324 mL
    10 mM 0.2116 mL 1.0581 mL 2.1162 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 25 mg/mL (52.91 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (5.29 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 1 mg/mL (2.12 mM); Clear solution

    *All of the co-solvents are available by MCE.
    References
    Kinase Assay
    [3]

    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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [3]

    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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3]

    Each experimental group (vehicle or linagliptin treatment) consists of 10 individual ob/ob mice (n=10). Animals are treated orally once a day (8:00 AM) by gastrogavage using vehicle (1% methylcellulose) or linagliptin (3 mg/kg body weight in 1% methylcellulose) beginning 2 days (day−2) before wounding. After wounding, animals are subsequently treated once a day throughout the 10-day healing period.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Purity: 99.97%

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    Product Name:
    Linagliptin
    Cat. No.:
    HY-10284
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