受注:045-509-1970 |
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Synonyms | LAF-237, NVP-LAF 237 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C17H25N3O2 |
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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) |
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* <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 | Vildagliptin inhibits DPP−4 with IC50 of 2.3 nM. |
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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. Vildagliptin 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 Vildagliptin (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] Vildagliptin(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] Vildagliptin 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] |
キナーゼアッセイ | DPP-IV Inhibition Measurement | |
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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). Vildagliptin 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 |
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 |
Dipeptidyl peptidase-IV inhibitors used in type-2 diabetes inhibit a phospholipase C: a case of promiscuous scaffolds in proteins. [Chakraborty S, et al. F1000 Res, 2014, 10.12688/f1000research.2-286.v1#sthash.jy5dbjcX.dpuf] |
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。
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