Linagliptin (GSK2118436)

製品コードS3031 バッチS303103

印刷

化学情報

Chemical Structure Synonyms BI-1356 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C25H28N8O2
分子量 472.54 CAS No. 668270-12-0
Solubility (25°C)* 体外 DMSO 24 mg/mL (50.78 mM)
Ethanol 7 mg/mL (14.81 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5% DMSO 40% PEG300 5%Tween80 50% ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 1.200mg/ml (2.54mM) Taking the 1 mL working solution as an example, add 50 μL of 24 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 0.600mg/ml (1.27mM) Taking the 1 mL working solution as an example, add 50 μL of 12 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <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.

溶剤液（一定の濃度）を調合する

生物活性

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.
in vitro

Linagliptin (GSK2118436) shows a potent inhibition effect against DPP-4 in vitro and a low affinity for hERG channel and M1 receptor (IC50 295 nM). [1] It 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

Linagliptin (GSK2118436) shows a highly efficacious, long-lasting, and potent inhibitory activity against DPP-4 by more than 70% inhibition in male Wistar rats, Beagle dogs, and Rhesus monkeys after oral administration of 1 mg/kg. Oral administration of this compound 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, it 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]

プロトコル(参考用のみ)

キナーゼアッセイ In Vitro DPP-4 Inhibition Assay
For determination of the in vitro potency of this compound, 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.

参考

  • https://pubmed.ncbi.nlm.nih.gov/18052023/
  • https://pubmed.ncbi.nlm.nih.gov/18223196/
  • https://pubmed.ncbi.nlm.nih.gov/22493041/
  • https://pubmed.ncbi.nlm.nih.gov/28813679/

カスタマーフィードバック

Data from [Data independently produced by , , Life Sci, 2018, 210:47-54]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Cooperative nutrient scavenging is an evolutionary advantage in cancer [ Nature, 2025, 10.1038/s41586-025-08588-w] PubMed: 39972131
CD26 acts as a host restriction factor to inhibit Influenza A virus (H1N1) infection [ Int J Biol Macromol, 2025, 330(Pt 3):148150] PubMed: 41067348
Targeting osteoclast-derived DPP4 alleviates inflammation-mediated ectopic bone formation in ankylosing spondylitis [ Arthritis Res Ther, 2025, 27(1):40] PubMed: 40001226
Cyclic tachyplesin I kills proliferative, non-proliferative and drug-resistant melanoma cells without inducing resistance [ Pharmacol Res, 2024, 207:107298] PubMed: 39032840
Patient-derived rhabdomyosarcoma cells recapitulate the genetic and transcriptomic landscapes of primary tumors [ iScience, 2024, 27(10):110862] PubMed: 39319271
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

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。