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。

Sitagliptin

CAS No. : 486460-32-6

MCE 站：Sitagliptin

产品活性：Sitagliptin (MK-0431) 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.?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：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

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。