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Sitagliptin phosphate monohydrate
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Sitagliptin phosphate monohydrate
CAS No. : 654671-77-9
MCE 站:Sitagliptin phosphate monohydrate
产品活性:Sitagliptin (MK0431 phosphate monohydrate) 是一种有效的 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.?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: 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:Drug Repurposing Compound Library Plus | FDA-Approved Drug Library Plus | FDA-Approved Drug Library Mini | Bioactive Compound Library Plus | Metabolism/Protease Compound Library | FDA-Approved Drug Library | Autophagy Compound Library | Drug Repurposing Compound Library | Diabetes Related Compound Library | Ferroptosis Compound Library | Anti-COVID-19 Compound Library | Orally Active Compound Library | FDA Approved & Pharmacopeial Drug Library | Drug-Induced Liver Injury (DILI) Compound Library | Talabostat mesylate | Puromycin aminonucleoside | Vildagliptin | 1G244 | Diprotin A TFA | Nateglinide | Prolyl Endopeptidase Inhibitor 1 | DPP-IV-IN-2 | Prodipine hydrochloride | Saikogenin A | UAMC00039 dihydrochloride | 2-Methoxy-5-acetoxy-fruranogermacr-1(10)-en-6-one | Azaleatin | Evogliptin tartrate | NDMC101 | NVP-DPP728 dihydrochloride | DPP-IV-IN-1
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