包装 | 价格(元) |
10mM (in 1mL DMSO) | 电议 |
200mg | 电议 |
500mg | 电议 |
Cell lines | Endothelial progenitor cells (EPCs) and bone marrow mesenchymalstem cells(MSC) |
Preparation method | The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. |
Reaction Conditions | 14 d; 25 μmol/L |
Applications | To determine whether sitagliptin treatment participated in enhancing the differentiation of EPCs and MSCs and cells expressing its ligand, SDF-1α, adipose tissues were co-cultured with sitagliptin (25 μmol/L) in M199 culture medium for 14 d and examined by flow cytometric analysis. The results show that compared with the 7 d cell culture, the numbers of EPCs [CD31/Sca-1+(double-stained) and CXCR4+ (single-stained)] were remarkably higher at day 14 in both the non-sitagliptin-treated (Si-T) group and the Si-T group |
Animal models | ApoE–/–mice with the C57BL/6 genetic background |
Dosage form | 200 mg/kg/day; oral taken |
Applications | In ApoE–/–mice, the sitagliptin group showed fewer atherosclerotic plaques than in controls (7.64±1.98% [range 4.62–10.13%] vs 12.91±1.15% [range 11.55–14.37%], p |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
产品描述 | Sitagliptin phosphate monohydrate is a potent inhibitor of DPP4 with IC50 of 19 nM in Caco-2 cell extracts. Sitagliptin phosphate exhibits a potent inhibitory effect on DPP-4 with IC50 of 19 nM from Caco-2 cell extracts[1]. Sitagliptin reduces in vitro migration of isolated splenic CD4 T-cells through a pathway involving cAMP/PKA/Rac1 activation[2]. 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[3]. 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[1]. 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[4]. 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[5]. References: |