(Rac)-Sitagliptin,823817-56-7

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

(Rac)-Sitagliptin

CAS No. : 823817-56-7

MCE 国际站：(Rac)-Sitagliptin

产品活性：(Rac)-Sitagliptin 是 Sitagliptin (HY-13749) 的一种异构体。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：Autophagy  |  Metabolic Enzyme/Protease

作用靶点：Autophagy  |  Dipeptidyl Peptidase

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.

相关产品：Puromycin aminonucleoside  |  Sitagliptin  |  Talabostat mesylate  |  Linagliptin  |  Brensocatib  |  Saxagliptin  |  1G244  |  Vildagliptin  |  Omarigliptin  |  Diprotin A  |  Teneligliptin  |  Nateglinide  |  Alogliptin  |  Trelagliptin  |  Anagliptin  |  Gemigliptin tartrate  |  DPP-IV-IN-2  |  Retagliptin phosphate  |  UAMC00039 dihydrochloride  |  DPP-IV-IN-1  |  Azaleatin  |  DBPR108  |  Dutogliptin  |  Evogliptin tartrate

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Dye Reagents  |  PROTAC  |  Isotope-Labeled Compounds