Vildagliptin

製品コードS3033 バッチS303302

印刷

化学情報

Chemical Structure Synonyms LAF-237, NVP-LAF 237 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C17H25N3O2
分子量 303.4 CAS No. 274901-16-5
Solubility (25°C)* 体外 DMSO 60 mg/mL (197.75 mM)
Water 60 mg/mL (197.75 mM)
Ethanol 60 mg/mL (197.75 mM)
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
Saline

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。

 30.000mg/ml (98.88mM) Taking the 1 mL working solution as an example, add 30 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, 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 Vildagliptin inhibits DPP−4 with IC50 of 2.3 nM.
in vitro

Vildagliptin is the most stable DPP-IV inhibitor, binding in the S1- and S2-catalytic sites of DPP-IV, possessing a P-1 site transition-state mimetic. [1]
in vivo

Vildagliptin (orally dosed with 10 μmol/kg) is a potent, orally active inhibitor of plasma DPP-IV activity that provides increased levels of GLP-1 in an oral glucose tolerance test (OGTT) with Obese male Zucker rats. This compound orally dosed with 10 μmol/kg both significantly decreases glucose excursions and stimulates insulin secretion in Obese male Zucker rats. Maximum inhibition of plasma DPP-IV activity (95%) is observed approximately 2 hours postdose of this compound (1 μmol/kg, po) while >50% inhibition of DPP-IV is observed within 30 min postdose and persisted for >10 hours in normal Cynomolgus monkeys. [1] This chemical (60 mg/kg) increases pancreatic beta cell mass through enhanced beta cell replication and reduced apoptosis, and the increased beta cell mass is sustained for 12 days after vildagliptin washout. [2] This compound administrated at doses of 10 mg/kg for 32 weeks protects nerve fiber loss in streptozotocin (STZ)-induced diabetic adult male Sprague Dawley rats. [3]

プロトコル(参考用のみ)

キナーゼアッセイ DPP-IV Inhibition Measurement
An extract from human colonic carcinoma cells (Caco-2) is used as the source of DPP-IV in the assay. The cells are differentiated to induce DPP-IV expression as described. Cell extract is prepared from cells solubilized in lysis buffer (10 mM Tris-HCl, 0.15 M NaCl, 0.04 T.I.U. (trypsin inhibitor unit) aprotinin, 0.5% nonidet-P40, pH 8.0) then centrifuged at 3.5×4g for 30 min at 4 °C to remove cell debris. The assay is conducted by adding 20 μg of solubilized Caco-2 protein, diluted to a final volume of 125 μL in assay buffer (25 mM Tris-HCl pH 7.4, 140 mM NaCl, 10 mM KCl, 1% bovine serum albumin) to 96-well flat-bottom microtiter plates. The reaction is initiated by adding 25 μL of 1 mM substrate. The reaction is run at room temperature for 10 min, and then 19 μL of 25% glacial acetic acid is added to stop the reaction. Fluorescence is measured using a CytoFluor II fluorometer (excitation 380 nm/ emission 460 nm). This compound and solvent controls are added as 30 μL additions, and the assay buffer volume is reduced to 95 μL.
動物実験 動物モデル Obese male Zucker rats
投薬量 10 μmol/kg
投与方法 Orally administrated at a single dose

参考

  • https://pubmed.ncbi.nlm.nih.gov/12801240/
  • https://pubmed.ncbi.nlm.nih.gov/21070766/
  • https://pubmed.ncbi.nlm.nih.gov/20082866/
  • https://pubmed.ncbi.nlm.nih.gov/20625970/

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：

CD26 Is Differentially Expressed throughout the Life Cycle of Infantile Hemangiomas and Characterizes the Proliferative Phase [ Int J Mol Sci, 2024, 25(18)9760] PubMed: 39337249
DPP4 inhibition impairs senohemostasis to improve plaque stability in atherosclerotic mice [ J Clin Invest, 2023, 133(12)e165933] PubMed: 37097759
Dipeptidyl peptidase 4 inhibition sensitizes radiotherapy by promoting T cell infiltration [ Oncoimmunology, 2023, 12(1):2268257] PubMed: 37849962
Non-Specific Inhibition of Dipeptidyl Peptidases 8/9 by Dipeptidyl Peptidase 4 Inhibitors Negatively Affects Mesenchymal Stem Cell Differentiation [ J Clin Med, 2023, 12(14)4632] PubMed: 37510747
Identification of circular RNAs and functional competing endogenous RNA networks in human proximal tubular epithelial cells treated with sodium-glucose cotransporter 2 inhibitor dapagliflozin in diabetic kidney disease [ Bioengineered, 2022, 13(2):3911-3929] PubMed: 35129424
Interrogation of kinase genetic interactions provides a global view of PAK1-mediated signal transduction pathways [ J Biol Chem, 2020, jbc.RA120.014831] PubMed: 33060198
Similarity and dissimilarity in antinociceptive effects of dipeptidyl-peptidase 4 inhibitors, Diprotin A and vildagliptin in rat inflammatory pain models following spinal administration [ Brain Res Bull, 2019, 147:78-85] PubMed: 30738866
The Tumor Suppressor p53 Limits Ferroptosis by Blocking DPP4 Activity [ Cell Rep, 2017, 20(7):1692-1704] PubMed: 28813679
Molecular cloning and biochemical characterization of Xaa-Pro dipeptidyl-peptidase from Streptococcus mutans and its inhibition by anti-human DPP IV drugs. [ FEMS Microbiol Lett, 2016, 363(9)] PubMed: 27010012
The dipeptidyl peptidase IV inhibitors vildagliptin and K-579 inhibit a phospholipase C: a case of promiscuous scaffolds in proteins. [Chakraborty S, et al. F1000 Res, 2015, 10.12688/f1000research.2-286.v3. eCollection 2013] PubMed: 25671081

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。