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/ Vildagliptin/维达列汀

Vildagliptin/维达列汀 {[allProObj[0].p_purity_real_show]}

货号：A403832 同义名： 维格列汀 / LAF237; NVP-LAF 237

Vildagliptin 是一种 DPP-4 抑制剂（IC50 2.3 nM），常用于 2 型糖尿病的研究。

Vildagliptin/维达列汀 化学结构 CAS号：274901-16-5
Vildagliptin/维达列汀 化学结构
CAS号：274901-16-5
Vildagliptin/维达列汀 3D分子结构
CAS号：274901-16-5
Vildagliptin/维达列汀 化学结构 CAS号：274901-16-5
Vildagliptin/维达列汀 3D分子结构 CAS号：274901-16-5
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Vildagliptin/维达列汀 纯度/质量文件 产品仅供科研

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全球学术期刊中引用的产品

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Vildagliptin/维达列汀 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].

Vildagliptin/维达列汀 细胞实验

Cell Line
Concentration Treated Time Description References
Human umbilical vein endothelial cells (HUVECs) High dose group: 240 mg/40 mg (PLGA/vildagliptin, w/w); Low dose group: 260 mg/20 mg (PLGA/vildagliptin, w/w) 14 days To evaluate the effect of vildagliptin on HUVECs migration. Results showed that both high and low doses of vildagliptin significantly promoted HUVECs migration (high dose group: 224±33%; low dose group: 161±34%). Int J Nanomedicine. 2019 Sep 13;14:7503-7513.
3T3-L1 adipocytes 1 nM, 10 nM, 100 nM 24 hours To assess the effect of vildagliptin and GLP-1 on adiponectin expression in 3T3-L1 adipocytes. Results showed that GLP-1 significantly increased adiponectin mRNA expression, while vildagliptin had no significant effect. J Biol Chem. 2014 Sep 26;289(39):27235-27245.
Human leukemia HL-60 cells 1 µM, 10 µM, 100 µM 24 hours To investigate the effect of vildagliptin on S100A8, S100A9, and TNF-α mRNA expression. Results showed that vildagliptin significantly induced the mRNA expression of S100A8 and S100A9 but had no significant effect on TNF-α mRNA expression. Sci Rep. 2016 Oct 19;6:35633.
Human hepatoma HepG2 cells 1 µM, 10 µM, 100 µM 24 hours To investigate the effect of vildagliptin on S100A9 and TNF-α mRNA expression. Results showed that vildagliptin increased the mRNA expression levels of S100A9 and TNF-α in a concentration-dependent manner. Sci Rep. 2016 Oct 19;6:35633.
Rat cardiac myoblast H9c2 cells 30 µM 48 hours To evaluate the effect of vildagliptin on autophagy in H9c2 cells under high glucose conditions. Results showed that vildagliptin restored autophagy levels, reduced P62 expression, and increased LC3 aggregation. Front Pharmacol. 2021 Mar 18;12:634365.
Rat cardiac myoblast H9c2 cells 30 µM 48 hours To evaluate the effect of vildagliptin on autophagy in H9c2 cells under high glucose conditions. Results showed that vildagliptin restored autophagy levels, reduced P62 expression, and increased LC3 aggregation. Front Pharmacol. 2021 Mar 18;12:634365.
Human umbilical vein endothelial cells (HUVECs) 1.0 µM 48 hours VLD significantly reduced mtROS production and mitochondrial DNA damage, enhanced ATP synthesis, reduced the expression of Drp1 and Fis1, blocked Drp1 translocation into mitochondria, and blunted mitochondrial fragmentation induced by hyperglycemia. J Cell Mol Med. 2019 Feb;23(2):798-810.
Human umbilical vein endothelial cells (HUVECs) 1 nM, 5 nM, 10 nM 6 hours To assess the effect of vildagliptin and/or GLP-1 on the formation of vascular-like structures by HUVECs on a Matrigel matrix. Results showed that treatment with vildagliptin or GLP-1 promoted the formation of vascular-like tubes, with GLP-1 being more effective. J Biol Chem. 2014 Sep 26;289(39):27235-27245.
Human lung microvascular endothelial cells (HMVEC-L) 10 nM 96 hours To evaluate the inhibitory effect of vildagliptin on LPS-induced endothelial-to-mesenchymal transition (EndMT) in the absence of immune cells or GLP-1. Results showed that vildagliptin significantly attenuated EndMT. Respir Res. 2017 Oct 16;18(1):177.

Vildagliptin/维达列汀 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
C57BL6/J mice Hind limb ischemia model Drinking water 0.6 mg/ml/day/mouse Administration started 3 days before surgery and continued for up to 3 weeks after surgery. To assess the effect of vildagliptin on ischemia-induced revascularization. Results showed that vildagliptin treatment significantly enhanced blood flow recovery and capillary density in the ischemic limbs of wild-type mice, but not in eNOS-deficient mice. J Biol Chem. 2014 Sep 26;289(39):27235-27245.
C57BL/6 mice Systemic endotoxemic lung injury model Intraperitoneal injection 10 mg/kg Once daily for 14 consecutive days To evaluate the ameliorative effect of vildagliptin on pulmonary fibrosis in a systemic endotoxemic lung injury model. Results showed that vildagliptin ameliorated pulmonary fibrosis by downregulating EndMT. Respir Res. 2017 Oct 16;18(1):177.
Mice C57BL/6NCrSlc mice Oral 1000 mg/kg Single dose, sampled after 24 hours To investigate the effect of vildagliptin on hepatic gene expression in mice. Results showed that vildagliptin significantly induced the mRNA expression of S100a8 and S100a9. Sci Rep. 2016 Oct 19;6:35633.
Mice Type 2 diabetic mouse model Oral gavage 15.17 mg/kg/day Once daily for 10 weeks To evaluate the effect of vildagliptin on cardiac function and autophagy in diabetic cardiomyopathy mice. Results showed that vildagliptin improved cardiac function, restored autophagy levels, and alleviated fibrosis. Front Pharmacol. 2021 Mar 18;12:634365.
Mice BKS.Cg-Dock7m+/+Leprdb/Nju (db/db) mice Oral 35 mg/kg Once daily for 6 weeks VLD significantly reduced blood glucose and serum triglyceride levels, decreased vascular ROS and mtROS production, increased NO generation, and inhibited the expression of Drp1 and Fis1, improving mitochondrial dysfunction in diabetic mice. J Cell Mol Med. 2019 Feb;23(2):798-810.
Sprague-Dawley rats Diabetic wound model Topical administration 40 mg vildagliptin with 240 mg PLGA 14 days Evaluate the effect of vildagliptin/PLGA nanofibrous membranes on diabetic wound healing, results showed accelerated wound closure and increased angiogenesis Pharmaceuticals (Basel). 2022 Nov 4;15(11):1358
Wistar albino rats 3-nitropropionic acid (3NP)-induced Huntington's disease model Oral 5 mg/kg/day Once daily for 14 days Vildagliptin attenuated Huntington's disease through activation of GLP-1 receptor/PI3K/Akt/BDNF pathway, improving cognitive and motor deficits, restoring mitochondrial function and oxidative stress balance, and modulating neurotransmitter levels. Neurotherapeutics. 2020 Jan;17(1):252-268
Asians Type 2 diabetes patients Oral 50 mg bid Twice daily for 24 weeks To assess the efficacy and safety of vildagliptin as add-on therapy to insulin in Asian patients with type 2 diabetes mellitus. Results showed that vildagliptin significantly reduced HbA1c without increasing the risk of hypoglycemia or weight gain. World J Diabetes. 2013 Aug 15;4(4):151-6
C57BL/6 mice MPTP-induced Parkinson’s disease model Oral 50 mg/kg Once per day for seven days To evaluate the protective effects of vildagliptin against MPTP-induced motor dysfunction, results showed that vildagliptin significantly improved MPTP-induced motor coordination deficits and motor learning impairment. Int J Mol Sci. 2022 Feb 21;23(4):2388
Mice KK-Ay diabetic mice and C57BL/6JJcl (B6) control mice Oral 50 mg/kg/day Once daily for 4 weeks Vildagliptin increases βcell mass by not only directly affecting cell kinetics but also by indirectly reducing cell apoptosis, oxidative stress and endoplasmic reticulum stress in diabetic mice. Diabetes Obes Metab. 2013 Feb;15(2):153-63
New Zealand white rabbits Diabetic model (induced by intravenous injection of alloxan) Local release (via stent implantation) High dose group: 240 mg/40 mg (PLGA/vildagliptin, w/w); Low dose group: 260 mg/20 mg (PLGA/vildagliptin, w/w) Single implantation, lasting for 8 weeks To evaluate the effect of vildagliptin-eluting stents on re-endothelialization and neointimal formation in diabetic rabbits. Results showed that both high and low doses of vildagliptin significantly promoted re-endothelialization (high dose group: 98.4±1.0%; low dose group: 95.4±1.1%) and reduced neointimal formation. Int J Nanomedicine. 2019 Sep 13;14:7503-7513.

Vildagliptin/维达列汀 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 <<

Vildagliptin/维达列汀 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

Vildagliptin/维达列汀 实验方案

计算器
存储液制备 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

Vildagliptin/维达列汀 技术信息

CAS号274901-16-5
分子式C17H25N3O2
分子量 303.4
SMILES Code O[C@@]1(C2)C[C@H]3C[C@H](C[C@]2(NCC(N4[C@H](C#N)CCC4)=O)C3)C1
MDL No. MFCD08275142
别名 维格列汀 ;LAF237; NVP-LAF 237; Zomelis; DSP 7238
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C
溶解方案

H2O: 50 mg/mL(164.8 mM)，配合低频超声助溶

配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案 一

Tags: Vildagliptin | 274901-16-5 | LAF237 | NVP-LAF 237 | LAF 237 | LAF-237 | DPP-IV Inhibitor | Metabolic Enzyme/Protease | Apoptosis | Dipeptidyl Peptidase | Ferroptosis | Apoptosis | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Vildagliptin/维达列汀 纯度/质量文件 | Vildagliptin/维达列汀 生物活性 | Vildagliptin/维达列汀 临床数据 | Vildagliptin/维达列汀 参考文献 | Vildagliptin/维达列汀 实验方案 | Vildagliptin/维达列汀 技术信息

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