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| 100mg |
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| 250mg |
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| 500mg |
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Purity: ≥98%
Linagliptin (formerly known as BI-1356; trade names Tradjenta and Trajenta) is a xanthine-based, highly potent, selective, and competitive DPP-4 inhibitor based on xanthine that may have anti-diabetic effects. At an IC50 of 1 nM, it inhibits DPP-4. The breakdown of incretins like GLP-1, which is crucial to the process of glucose metabolism, is largely mediated by DPP-4. DPP-4, which is found on the capillary endothelium close to the L-cells where GLP-1 is secreted in the ileum, quickly truncates GLP-1 under physiological conditions. The FDA approved linagliptin on May 2, 2011, for the treatment of type II diabetes. Lilly and Boehringer Ingelheim are the companies marketing it.
| Targets |
Ferroptosis; DPP-4 (IC50 = 1 nM)
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| ln Vitro |
Linagliptin has a low affinity for the hERG channel and M1 receptor (IC50 295 nM) and a strong inhibitory effect against DPP-4 in vitro.[1] Linagliptin exhibits 10,000-fold higher selectivity for DPP-4 than DPP-8, DPP-9, amino-peptidases N and P, prolyloligopeptidase, trypsin, plasmin, and thrombin, as well as 90-fold higher selectivity than fibroblast activation protein in vitro. Furthermore, it functions as a competitive inhibitor with a Ki of 1 nM.[2]
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| ln Vivo |
Linagliptin demonstrates a highly effective, prolonged, and potent inhibitory activity against DPP-4 by more than 70% inhibition for all three species following oral administration of 1 mg/kg in male Wistar rats, Beagle dogs, and Rhesus monkeys. When Linagliptin is given orally to db/db mice 45 minutes prior to an oral glucose tolerance test, plasma glucose excursion decreases from 0.1 mg/kg (15% inhibition) to 1 mg/kg (66% inhibition) in a dose-dependent manner.[1] Linagliptin inhibits DPP-4 activity, which decreases the expression of proinflammatory markers such as macrophage inflammatory protein-2 and cyclooxygenase-2. Additionally, it increases the formation of myofibroblasts in wound healing from ob/ob mice.[3]
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| Enzyme Assay |
The EDTA plasma (20 μL) is combined with 50 μL of H-Ala-Pro-7-amido-4-trifluoromethylcoumarin after being diluted with 30 μL of DPP-4 assay buffer (100 mM Tris and 100 mM NaCl, pH 7.8 corrected with HCl). To get a final concentration of 100 μM, the 200 mM stock solution in dimethylformamide is diluted 1:1000 with water. After 10 minutes of room temperature incubation, the fluorescence in the wells is measured using a Victor 1420 Multilabel Counter set to 405 nm for excitation and 535 nm for emission. In place of 20 μL of plasma, 100 μg of protein from the corresponding wound lysates is used to detect DPP-4 activity in the lysates. Utilizing the Mouse/Rat Total Active GLP-1 Assay Kit, active GLP-1 is also identified in 100 μg of the corresponding wound tissue samples.
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| Cell Assay |
In 24-well plates, 4.0×107 keratinocytes are seeded per well. Following 50% confluence, cells are starved with DMEM for a full day. Using 1 μCi/mL of [3H]methyl-thymidine in DMEM with 10% fetal bovine serum and varying concentrations of linagliptin (3, 30, 300, or 600 nM) for 24 hours, the proliferation of cells is measured. Following two rounds of washing with phosphate-buffered saline, the cells are incubated for 30 minutes at 4°C in 5% trichloroacetic acid. Subsequently, the DNA is solubilized for 30 minutes at 37°C in 0.5mol/LNaOH. At last, the incorporation of [3H]thymidine is found.
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| Animal Protocol |
There are ten separate ob/ob mice (n=10) in each experimental group (car or linagliptin treatment). Animals are given oral treatment once a day (8:00 AM) either with linagliptin (3 mg/kg body weight in 1% methylcellulose) or vehicle (1% methylcellulose) starting two days (day−2) prior to wounding. Animals that have been wounded are then given treatment once a day for ten days.
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| References |
| Molecular Formula |
C25H28N8O2
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|---|---|
| Molecular Weight |
472.54
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| Exact Mass |
472.23
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| Elemental Analysis |
C, 63.54; H, 5.97; N, 23.71; O, 6.77
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| CAS # |
668270-12-0
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| Related CAS # |
Linagliptin-d4;2140263-92-7;Linagliptin-13C,d3;1398044-43-3
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| Appearance |
Solid powder
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| SMILES |
CC#CCN1C2=C(N=C1N3CCC[C@H](C3)N)N(C(=O)N(C2=O)CC4=NC5=CC=CC=C5C(=N4)C)C
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| InChi Key |
LTXREWYXXSTFRX-QGZVFWFLSA-N
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| 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
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| Chemical Name |
8-[(3R)-3-aminopiperidin-1-yl]-7-but-2-ynyl-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]purine-2,6-dione
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| Synonyms |
Linagliptin; BI-1356; BI1356; BI 1356; trade names: Tradjenta, Trajenta
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 25 mg/mL (52.91 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 250.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: 2.5 mg/mL (5.29 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.29 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 0.5% hydroxyethyl cellulose: 30 mg/mL |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05200793 | Recruiting | Drug: Empagliflozin 25 mg Drug: Linagliptin 10 mg |
Polycystic Ovary Syndrome (PCOS) |
Alexandria University | December 7, 2021 | Phase 4 |
| NCT06098625 | Not yet recruiting | Drug: Linagliptin 5 mg Oral Tablet Drug: Empagliflozin 25 MG |
Diabetes Mellitus | Medanta, The Medicity, India | November 10, 2023 | Not Applicable |
| NCT06095492 | Not yet recruiting | Drug: Empagliflozin 25 MG Drug: Linagliptin |
Diabetes Mellitus | Medanta, The Medicity, India | October 30, 2023 | Not Applicable |
| NCT05130463 | Active Recruiting |
Drug: empagliflozin/linagliptin | Diabetes Mellitus, Type 2 | Boehringer Ingelheim | March 22, 2022 | |
| NCT04670666 | Not yet recruiting | Other: METFORMIN PLACEBO Drug: METFORMIN |
Type 2 Diabetes Mellitus | EMS | August 2023 | Phase 3 |
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