| Description | Anagliptin (SK-0403) is a potent Inhibitor of DPP-4(IC50 of 3.8 nM), for the treatment of type 2 diabetes mellitus. |
| In vitro | 可溶性DPP-4促进了培养的SMC增殖，而anagliptin通过抑制ERK磷酸化作用抑制了该增殖。在THP-1细胞中，anagliptin通过抑制ERK磷酸化和核因子-κB的核内转移，减少了脂多糖诱导的TNF-α产生。量化分析还显示，anagliptin减少了apoE缺陷小鼠[1]中动脉粥样硬化病变的面积。 |
| In vivo | 连续使用anagliptin 16周显著减少了血管壁中单核细胞和巨噬细胞的积聚、斑块区域的平滑肌细胞（SMC）含量以及主动脉瓣周围的油红O染色区域，而不影响葡萄糖耐受性或体重。血清DPP-4浓度在apoE缺陷小鼠中显著高于对照小鼠，并且随着年龄的增长水平上升，这表明DPP-4参与了动脉粥样硬化的进展。anagliptin治疗显著降低了血浆总胆固醇（降低14%，P < 0.01）和甘油三酯水平（降低27%，P < 0.01）。低密度脂蛋白胆固醇和极低密度脂蛋白胆固醇的水平也通过anagliptin治疗显著降低。anagliptin处理的小鼠在夜间固醇调节元件结合蛋白-2信使核糖核酸表达水平显著降低（降低15%，P < 0.05）。在HepG2细胞中，anagliptin显著抑制了固醇调节元件结合蛋白活性（降低21%，P < 0.001）。 |
| Animal experiments | Male low-density lipoprotein receptor-deficient mice were administered 0.3% anagliptin in their diet.?Plasma lipid levels were assayed and lipoprotein profile was analyzed using high-performance liquid chromatography.?Hepatic gene expression was examined by deoxyribonucleic acid microarray and quantitative polymerase chain reaction analyses[2]. |
| Target activity | DPP8:68 nM , DPP9:60 nM, DPP4:3.8 nM |
| Synonyms | SK-0403, 阿拉格列汀 |
| molecular weight | 383.45 |
| Molecular formula | C19H25N7O2 |
| CAS | 739366-20-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 50 mg/mL (130.4 mM), Sonication is recommended. |
| References | 1. Ervinna N, et al. Anagliptin, a DPP-4 inhibitor, suppresses proliferation of vascular smooth muscles and monocyte inflammatory reaction and attenuates atherosclerosis in male apo E-deficient mice. Endocrinology. 2013 Mar;154(3):1260-70. 2. Yano W, et al. Mechanism of lipid-lowering action of the dipeptidyl peptidase-4 inhibitor, anagliptin, in low-density lipoprotein receptor-deficient mice. J Diabetes Investig. 2017 Mar;8(2):155-160. |