Vildagliptin

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Chemical Structure| 274901-16-5 同义名 : 维格列汀 ;LAF237;NVP-LAF 237;Zomelis;DSP 7238
CAS号 : 274901-16-5
货号 : A403832
分子式 : C17H25N3O2
纯度 : 98%
分子量 : 303.399
MDL号 : MFCD08275142
存储条件：

Pure form Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

H2O: 50 mg/mL(164.8 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 Vildagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor. It improves glycaemic control by inhibiting DPP-4 from inactivating the incretin hormones glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide, prolonging incretin activity in response to ingestion of nutrients. Vildagliptin also showed efficacy in reducing HbA(1c) levels in patients with type 2 diabetes when used in combination with metformin, pioglitazone or insulin. Vildagliptin was generally well tolerated when administered alone or in combination with additional antidiabetic treatment[3]. Oral vildagliptin is a useful option as monotherapy or as add-on therapy for patients with type 2 diabetes[4]. Inhibiting DPP-4 (dipeptidyl peptidase) signaling by vildagliptin could ameliorate pulmonary fibrosis by downregulating EndMT in systemic LPS-induced lung injury[5]. Vildagliptin (35 mg/kg; once daily by oral gavage) increases plasma active GLP-1 levels in islets of db/db mice[6]. Vildagliptin displayed protective capabilities against TNF-α-induced chondrocyte cell cycle arrest in the G1 phase. Moreover, vildagliptin suppresses the three major TNF-α-induced chondrocyte senescence proteins including p53, p21, and plasminogen activator inhibitor-1 (PAI-1). Vildagliptin also suppresses TNF-α-induced p53 acetylation at K382[7].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
Caco-2 cells Function assay Inhibition of human DPP4 expressed in Caco-2 cells, Ki=0.004 μM 17034148
insect cells Function assay Inhibition of human recombinant His-tagged DPP4 expressed in insect cells, IC50=0.056 μM 20718420
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01582308 Type 2 Diabetes Mellitus Phase 1 Completed - -
NCT01582308 - Completed - -
NCT00099931 Diabetes Mellitus, Type 2 Phase 3 Completed - Germany ... 展开 >> Novartis Investigative Site Investigative Sites, Germany 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.30mL

0.66mL

0.33mL

16.48mL

3.30mL

1.65mL

32.96mL

6.59mL

3.30mL
参考文献

[1]Duttaroy A, Voelker F, et al. The DPP-4 inhibitor vildagliptin increases pancreatic beta cell mass in neonatal rats. Eur J Pharmacol. 2011 Jan 15;650(2-3):703-7.

[2]Villhauer EB, Brinkman JA, et al. 1-[[(3-hydroxy-1-adamantyl)amino] acetyl] -2-cyano-(S)-pyrrolidine: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties. J Med Chem. 2003 Jun 19;46(13):2774-89.

[3]Henness S, Keam SJ. Vildagliptin. Drugs. 2006;66(15):1989-2001; discussion 2002-4

[4]Keating GM. Vildagliptin: a review of its use in type 2 diabetes mellitus. Drugs. 2014 Apr;74(5):587-610

[5]Suzuki T, Tada Y, Gladson S, Nishimura R, Shimomura I, Karasawa S, Tatsumi K, West J. Vildagliptin ameliorates pulmonary fibrosis in lipopolysaccharide-induced lung injury by inhibiting endothelial-to-mesenchymal transition. Respir Res. 2017 Oct 16;18(1):177

[6]Wu YJ, Guo X, Li CJ, Li DQ, Zhang J, Yang Y, Kong Y, Guo H, Liu DM, Chen LM. Dipeptidyl peptidase-4 inhibitor, vildagliptin, inhibits pancreatic beta cell apoptosis in association with its effects suppressing endoplasmic reticulum stress in db/db mice. Metabolism. 2015 Feb;64(2):226-35

[7]Bi J, Cai W, Ma T, Deng A, Ma P, Han Y, Lou C, Wu L. Protective effect of vildagliptin on TNF-α-induced chondrocyte senescence. IUBMB Life. 2019 Jul;71(7):978-985