Sitagliptin Phosphate Monohydrate 654671-77-9

Sitagliptin phosphate (trade name Januvia, code MK-0431), abbreviated as Sitagliptin, is produced by Merck Corporation in the United States. It was approved for sale by the US Food and Drug Administration (FDA) in October 2006 for the treatment of type 2 diabetes in Chemicalbook urine disease. The effect of cetagliptin phosphate on type 2 diabetes is very ideal. As a new anti diabetes drug, cetagliptin phosphate is glucose dependent and has moderate hypoglycemic effect. It can increase insulin secretion without hypoglycemia, effectively reduce hunger and other advantages, and has no side effects such as nausea, vomiting, edema and increasing body mass.

DPP-4, also known as CD26, exists on the surface of T cells and plays an important role in the immune system. DPP-4 can not only degrade Increlin, but also many other substances, such as growth hormone releasing hormone (GHRH), neuropeptide Y, pituitary adenylate cycle-activating peptide (PACAP), gastrin releasing peptide (GRP), etc. The half-life of lncretin in the body is very short and can be quickly degraded by DPP-4. The tv2 of GLP-1 in plasma is ≈ 1 minute. There are two main aspects of research on Increment. Firstly, the development of GLP-1 analogues that cannot be degraded by DPP-4 and have GLP-1 activity. As approved by the US FDA in 2005, enalapide is a GLChemicalbookP-1 receptor agonist, a non degradable peptide injected subcutaneously. The second is to develop inhibitors of DPP-4, and sitagliptin is one of them. Sitagliptin can inhibit DPP-4, increase the activity of GLP-1 and GIP in plasma, and slightly increase their content. Therefore, while exerting its hypoglycemic effect, it does not cause side effects such as nausea and vomiting caused by excessive GLP-1 content. Due to its glucose dependent stimulation of insulin secretion, it can greatly reduce the incidence of hypoglycemia caused by oral hypoglycemic drugs. In addition, the action of sitagliptin is highly selective. Research has found that its selectivity for DPP-4 is about 2600 times higher than DPP-8 and DPP-9, so side effects caused by the inhibition of DPP-8 and DPP-9 are rare.