Sitagliptin phosphate monohydrate,MK-0431是一种口服高效、高选择性DPP4抑制剂（IC₅₀ = 19 nM）,通过竞争性抑制机制（Kᵢ = 1 nM）阻断DPP-4对胰高血糖素样肽-1（GLP-1）和葡萄糖依赖性胰岛素多肽（GIP）的降解,从而提高活性肠促胰岛素水平。此外,该化合物可不依赖DPP-4,直接通过激活cAMP/PKA和ERK1/2通路刺激肠道L细胞分泌GLP-1。在1型糖尿病模型中,西格列汀磷酸盐一水合物对胰岛移植物具有保护作用,适用于1型及2型糖尿病的研究。
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英文别名 (English Synonym) |
Sitagliptin phosphate monohydrate |
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中文名称 (Chinese Name) |
西他列汀磷酸盐一水合物；西格列汀磷酸盐一水合物 |
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靶点 (Target) |
DPP-4 |
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通路 (Pathway) |
Protease/Metabolic Enzyme |
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CAS号 (CAS NO.) |
654671-77-9 |
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分子式 (Formula) |
C16H15F6N5O·H3PO4·H2O |
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分子量 (Molecular Weight) |
523.3 |
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纯度 (Purity) |
≥98% |
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溶解性 (Solubility) |
溶于DMSO |
-25~-15℃保存，有效期3年
[1] 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.[2]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.
