Dapagliflozin (BMS-512148) is a glucose co-transporter protein 2 (SGLT2) inhibitor that competitively binds to its target. Dapagliflozin is used in the treatment of type 2 diabetes mellitus and decreases glucose reabsorption in the kidneys and increases urinary excretion of glucose, which results in lowering plasma glucose levels.

SGLT2 (human):1.1 nM(EC50)

方法：人近端小管上皮细胞系 HK2 在常氧和缺氧条件下用 Dapagliflozin (1-10 µM) 处理 24 h，使用 Trypan blue staining 检测细胞活力。
结果：Dapagliflozin 预处理对常氧 HK2 细胞的细胞存活没有影响。与对照细胞相比，缺氧显著降低了 HK2 细胞的细胞活力，Dapagliflozin 预处理缺氧 HK2 细胞以剂量依赖的方式显著提高了细胞活力。[1]
方法：人近端小管上皮细胞系 HK2 用 Dapagliflozin (0.1 µM) 和 H2O2 (200 µM) 处理 24 h，使用 Hoechst 33342 和 PI 检测细胞凋亡。
结果：Dapagliflozin 显著降低了 H2O2 诱导的凋亡细胞死亡的百分比。Dapagliflozin 对 H2O2 诱导的细胞死亡有保护作用。[2]

方法：为研究对糖尿病动脉粥样硬化的影响，将 Dapagliflozin (1 mg/kg) 灌胃给药给高脂饮食诱导动脉粥样硬化的糖尿病 ApoE-/- 小鼠，每天一次，持续 12 周。
结果：Dapagliflozin 可能对高脂饮食诱导的糖尿病动脉粥样硬化具有治疗潜力，这些益处可能取决于通过 ROS-NLRP3-caspase-1 途径抑制巨噬细胞分泌 IL-1β 的作用。[3]

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.