受注:045-509-1970 |
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Synonyms | BI-1356 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C25H28N8O2 |
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分子量 | 472.54 | CAS No. | 668270-12-0 | |
Solubility (25°C)* | 体外 | DMSO | 17 mg/mL (35.97 mM) | |
Ethanol | 1 mg/mL (2.11 mM) | |||
Water | Insoluble | |||
* <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. |
製品説明 | Linagliptin (GSK2118436) is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM and exhibits a 10,000-fold higher selectivity for DPP-4 than for other dipeptidyl peptidases such as DPP-2, DPP-8, and DPP-9. Linagliptin activates glomerular autophagy in a model of type 2 diabetes. DPP4 mediates ferroptosis in TP53-deficient CRC cells. |
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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] |
キナーゼアッセイ | In Vitro DPP-4 Inhibition Assay | |
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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). | ||
動物実験 | 動物モデル | Male db/db mice |
投薬量 | ≤1 mg/kg | |
投与方法 | Administered via p.o. |
Data from [Data independently produced by , , Life Sci, 2018, 210:47-54]
Crosstalk with lung fibroblasts shapes the growth and therapeutic response of mesothelioma cells [ Cell Death Dis, 2023, 10.1038/s41419-023-06240-x] | PubMed: 37938546 |
Establishment and Characterization of NCC-PMP1-C1: A Novel Patient-Derived Cell Line of Metastatic Pseudomyxoma Peritonei [ J Pers Med, 2022, 12(2)258] | PubMed: 35207746 |
Establishment and characterization of NCC-UPS4-C1: a novel cell line of undifferentiated pleomorphic sarcoma from a patient with Li-Fraumeni syndrome [ Hum Cell, 2022, 10.1007/s13577-022-00671-y] | PubMed: 35118583 |
Linagliptin ameliorates pulmonary fibrosis in systemic sclerosis mouse model via inhibition of endothelial-to-mesenchymal transition [ Mol Cell Biochem, 2022, 477(4):995-1007] | PubMed: 34988855 |
Establishment and characterization of the NCC-GCTB4-C1 cell line: a novel patient-derived cell line from giant cell tumor of bone [ Hum Cell, 2021, 10.1007/s13577-021-00639-4] | PubMed: 34731453 |
Establishment and characterization of NCC-MFS4-C1: a novel patient-derived cell line of myxofibrosarcoma [ Hum Cell, 2021, 34(6):1911-1918] | PubMed: 34383271 |
Establishment and characterization of novel patient-derived cell lines from giant cell tumor of bone [ Hum Cell, 2021, 10.1007/s13577-021-00579-z] | PubMed: 34304386 |
Targeting TRAF3IP2 alleviates high glucose-induced cardiomyocyte inflammation and apoptosis [ Drug Dev Res, 2021, 10.1002/ddr.21856] | PubMed: 34260107 |
Establishment and characterization of patient-derived cancer models of malignant peripheral nerve sheath tumors. [ Cancer Cell Int, 2020, 19;20:58] | PubMed: 32099531 |
Glucocorticoids mobilize macrophages by transcriptionally up-regulating the exopeptidase DPP4. [ J Biol Chem, 2020, 10.1074/jbc.RA119.010894] | PubMed: 31988243 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。