Sitagliptin phosphate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Sitagliptin 磷酸盐是一种二肽基肽酶 4 (DPP4) 抑制剂。

Sitagliptin phosphate is a dipeptidyl peptidase-4 (DPP4) inhibitor.(In Vitro):Sitagliptin phosphate potently inhibits DPP-4 in Caco-2 cell extracts with IC50 of 19 nM . Sitagliptin reduces in vitro migration of isolated splenic CD4 T cells through a pathway involving cAMP/PKA/Rac1 activation.(In Vivo):In free-fed Han-Wistar rats, the ED50 values ??for the inhibition of plasma DPP-4 activity by sitagliptin phosphate were calculated as 7 hours post-dose at 2.3 mg/kg and 24 hours post-dose at 30 mg/kg . A mouse model of streptozotocin-induced type 1 diabetes showed elevated plasma DPP-4 levels, which was significantly suppressed in mice on a sitagliptin phosphate diet. This is achieved through a positive effect on hyperglycemia regulation, possibly by prolonging islet graft survival. The plasma clearance and volume of distribution of sitagliptin phosphate in rats (40-48 mL/min/kg, 7-9 L/kg) were higher than those in dogs (9 mL/min/kg, 3 L/kg); its The half-life is shorter in rats, 2 hours in dogs and 4 hours in dogs.

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.?A recent study demonstrates that sitagliptin 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 therefore reduces the effect of autoimmunity on graft survival.

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.

Januvia | MK-0431 phosphate

Metabolic Enzyme/Protease

DPP

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654671-78-0

505.314

C16H18F6N5O5P

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (197.90 mM)

[H][H].OOP(=O)=O.N[C@@H](CC(=O)N1CCn2c(C1)nnc2C(F)(F)F)Cc1cc(F)c(F)cc1F

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(-20℃)

With Ice Pack

≥ 2 years