Vildagliptin
Vildagliptin is an inhibitor of dipeptidyl peptidase IV (DPP4) that increases levels of glucagon-like peptide 1 (GLP-1). Vildagliptin’s inhibition of DPP4 results in anti-diabetic and anti-hyperglycemic benefits, including increases in serum insulin and β-cell mass, decreases in serum glucagon, restoration of insulin/IGF1 signaling, and improved endoplasmic reticular stress in animal models. Additionally, this compound displays neuroprotective and cognition enhancing activities, attenuating amyloid-β (Aβ) pathology, tau phosphorylation, and release of inflammatory markers as well as improving memory retention in animal models; this indicates potential benefit as a treatment for Alzheimer’s disease with further investigation.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18978954
| Cas No. |
274901-16-5 |
|---|---|
| Purity |
≥97% |
| Formula |
C17H25N3O2 |
| Formula Wt. |
303.40 |
| IUPAC Name |
1-[2-[(3-hydroxy-1-adamantyl)amino]acetyl]pyrrolidine-2-carbonitrile |
| Synonym |
(2S)-(((3-Hydroxyadamantan-1-yl)amino)acetyl)pyrrolidine-2-carbonitrile; Galvus; (2R)-1-(2-((3-Hydroxy-1-adamantyl)amino)acetyl)pyrrolidine-2-carbonitrile; 1-(2-((3-Hydroxy-1-adamantyl)amino)acetyl)pyrrolidine -2-carbonitrile |
| Melting Point |
148-152°C |
| Appearance |
White to off white powder |
Kosaraju J, Murthy V, Khatwal RB, et al. Vildagliptin: an anti-diabetes agent ameliorates cognitive deficits and pathology observed in streptozotocin-induced Alzheimers disease. J Pharm Pharmacol. 2013 Dec;65(12):1773-84. PMID: 24117480.
Shimizu S, Hosooka T, Matsuda T, et al. DPP4 inhibitor vildagliptin preserves β-cell mass through amelioration of endoplasmic reticulum stress in C/EBPB transgenic mice. J Mol Endocrinol. 2012 Aug 30;49(2):125-35. PMID: 22822047.
Thornberry NA, Gallwitz B. Mechanism of action of inhibitors of dipeptidyl-peptidase-4 (DPP-4). Best Pract Res Clin Endocrinol Metab. 2009 Aug;23(4):479-86. PMID: 19748065.
Balas B, Baig MR, Watson C, et al. The dipeptidyl peptidase IV inhibitor vildagliptin suppresses endogenous glucose production and enhances islet function after single-dose administration in type 2 diabetic patients. J Clin Endocrinol Metab. 2007 Apr;92(4):1249-55. PMID: 17244786.
