Sitagliptin是口服高效高选择性二肽基肽酶4(DPP-4)抑制剂，通过竞争性抑制机制阻断DPP-4降解胰高血糖素样肽-1(GLP-1)和葡萄糖依赖性胰岛素多肽(GIP)，升高活性肠促胰岛素水平；还可独立于DPP-4，通过激活cAMP/PKA及ERK1/2通路直接刺激肠道L细胞分泌GLP-1。该药物可保护1型糖尿病模型中的胰岛移植物，适用于1型和2型糖尿病研究，临床用于2型糖尿病治疗。
| 英文别名 (English Synonym) | Sitagliptin |
| 中文名称 (Chinese Name) | 西格列汀；西他列汀 |
| 靶点 (Target) | DPP-4 |
| 通路 (Pathway) | Protease/Metabolic Enzyme |
| CAS号 (CAS NO.) | 486460-32-6 |
| 分子式 (Formula) | C16H15F6N5O |
| 分子量 (Molecular Weight) | 407.32 |
| 纯度 (Purity) | ≥98% |
| 溶解性 (Solubility) | 溶于DMSO |
-25~-15℃保存，有效期3年
[1] Thomas L, Eckhardt M, Langkopf E, Tadayyon M, Himmelsbach F, Mark M. (R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione (BI 1356), a novel xanthine-based dipeptidyl peptidase 4 inhibitor, has a superior potency and longer duration of action compared with other dipeptidyl peptidase-4 inhibitors. J Pharmacol Exp Ther. 2008 Apr;325(1):175-82. doi: 10.1124/jpet.107.135723. Epub 2008 Jan 25. PMID: 18223196.[2]Kim SJ, Nian C, Doudet DJ, McIntosh CH. Dipeptidyl peptidase IV inhibition with MK0431 improves islet graft survival in diabetic NOD mice partially via T-cell modulation. Diabetes. 2009 Mar;58(3):641-51. doi: 10.2337/db08-1101. Epub 2008 Dec 10. PMID: 19073764; PMCID: PMC2646063.[3]Sangle GV, Lauffer LM, Grieco A, Trivedi S, Iakoubov R, Brubaker PL. Novel biological action of the dipeptidylpeptidase-IV inhibitor, sitagliptin, as a glucagon-like peptide-1 secretagogue. Endocrinology. 2012 Feb;153(2):564-73. doi: 10.1210/en.2011-1732. Epub 2011 Dec 20. PMID: 22186413.[4]Kim SJ, Nian C, Doudet DJ, McIntosh CH. Inhibition of dipeptidyl peptidase IV with sitagliptin (MK0431) prolongs islet graft survival in streptozotocin-induced diabetic mice. Diabetes. 2008 May;57(5):1331-9. doi: 10.2337/db07-1639. Epub 2008 Feb 25. PMID: 18299314.[5]Beconi MG, Reed JR, Teffera Y, Xia YQ, Kochansky CJ, Liu DQ, Xu S, Elmore CS, Ciccotto S, Hora DF, Stearns RA, Vincent SH. Disposition of the dipeptidyl peptidase 4 inhibitor sitagliptin in rats and dogs. Drug Metab Dispos. 2007 Apr;35(4):525-32. doi: 10.1124/dmd.106.013110. Epub 2007 Jan 12. PMID: 17220241.
