Sitagliptin西格列汀,486460-32-6

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Sitagliptin

CAS No. : 486460-32-6

MCE 国际站：Sitagliptin

产品活性：Sitagliptin (MK-0431) 是一种有效的，具有口服活性的 DPP4 抑制剂，在 Caco-2 细胞中，IC₅₀ 值为 19 nM。

研究领域：Metabolic Enzyme/Protease  |  Autophagy

作用靶点：Dipeptidyl Peptidase  |  Autophagy

In Vitro: Sitagliptin phosphate exhibits a potent inhibitory effect on DPP-4 with IC₅₀ of 19 nM from Caco-2 cell extracts. Sitagliptin reduces in vitro migration of isolated splenic CD4 T-cells through a pathway involving cAMP/PKA/Rac1 activation. Stagliptin exerts a novel, direct action in order to stimulate GLP-1 secretion by the intestinal L cell through a DPP-4-independent, protein kinase A- and MEK-ERK1/2-dependent pathway. It reduces the effect of autoimmunity on graft survival.

In Vivo: In vivo, the ED₅₀ value of sitagliptin phosphate for inhibition of plasma DPP-4 activity is calculated to be 2.3 mg/kg 7 hour postdose and 30 mg/kg 24 hour postdose in freely fed Han-Wistar rats. The streptozotocin-induced type 1 diabetes mouse model exhibits elevated DPP-4 levels in the plasma that can be substantially inhibited in mice on an Sitagliptin phosphate diet. This is achieved by a positive effect on the regulation of hyperglycemia, potentially through prolongation of islet graft survival. The plasma clearance and volume of distribution of Sitagliptin phosphate are higher in rats (40-48 mL/min/kg, 7-9 L/kg) than in dogs (9 mL/min/kg, 3 L/kg); and its half-life is shorter in rats,2 hours compared with 4 hours in dogs.

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