Dapagliflozin竞争性的葡萄糖协同转运蛋白2 (SGLT2) 抑制剂,可促进尿液中葡萄糖的排泄,在糖尿病 (DM) 研究中具有价值。Dapagliflozin 诱导HIF1表达并减轻肾脏 IR 损伤。
产品描述
Dapagliflozin is a selective sodium-glucose co-transporter subtype 2 (SGLT2) inhibitor with antihyperglycemic activity.
体外活性
在高血糖链脲佐菌素大鼠中,口服 Dapagliflozin(0.1 mg/kg)能够降低血糖水平.在Zucker糖尿病肥胖大鼠中,Dapagliflozin对于肝脏和肾脏表现出良好的安全性,能够降低葡萄糖水平.
体内活性
在体外代谢通路中,Dapagliflozin能够参与糖脂化,羟乙基化,脱乙基作用。在大鼠,犬,猴,人类血清中,Dapagliflozin(10 μM )能够稳定发挥作用。在无蛋白buffer中,Dapagliflozin(20 μM)能够选择性地作用于GLUT转运蛋白
细胞实验
To perform the cell survival assay, cells are collected after 24 h incubation with vehicle or dapagliflozin pretreatment in 30-min ischemia and surviving cells are counted with Trypan blue staining. The percentage survival is determined by quantization of the relative viable number of treated cells divided by the viable number of untreated cells.
Cas No.
461432-26-8
分子式
C21H25ClO6
分子量
408.87
别名
达格列净;BMS-512148
储存和溶解度
H2O:<1 mgml
Ethanol:14 mg/mL (34.2 mM)
DMSO:76 mg/mL (185.9 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years