Linagliptin

SKU: orb1310851

Description

Linagliptin

Research Area

Cell Biology, Protein Biochemistry

Key Properties

• CAS Number: 668270-12-0
• MW: 472.54
• Purity: 99.15%
• Formula: C₂₅H₂₈N₈O₂
• SMILES: C(C#CC)N1C2=C(N=C1N3C[C@H](N)CCC3)N(C)C(=O)N(CC4=NC5=C(C(C)=N4)C=CC=C5)C2=O
• Target: Proteasome,Autophagy,DPP-4,Ferroptosis
• Solubility: DMSO:26.67 mg/mL (56.44 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.12 mM);Ethanol:1 mg/mL (2.12 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  DPP4:1 nM
• In Vivo:
  In male Wistar rats, Beagle dogs, and Rhesus monkeys, Linagliptin exhibits highly efficacious, long-lasting, and potent inhibitory activity against DPP-4 with over 70% inhibition for all three species after oral administration of 1 mg/kg. In db/db mice, oral administration of Linagliptin 45 min before an oral glucose tolerance test reduces plasma glucose excursion in a dose-dependent manner, achieving 15% inhibition at 0.1 mg/kg and 66% inhibition at 1 mg/kg. By inhibiting DPP-4 activity, Linagliptin also reduces the expression of the proinflammatory markers cyclooxygenase-2 and macrophage inflammatory protein-2, and enhances myofibroblast formation in healing wounds from ob/ob mice.
• 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). 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.
• Cell Research:
  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.

Storage & Handling

• Storage: keep away from direct sunlight,store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Dipeptidyl Peptidase, DPP, DPP4, DPP-4, Autophagy, BI 1356, BI1356, BI-1356, Inhibitor, Ferroptosis, inhibit, Linagliptin

Compound Identifiers

PubChem CID

10096344