| Description | Saxagliptin hydrate (Onglyza hydrate) is a selective and reversible DPP4 inhibitor (IC50: 26 nM; Ki: 1.3 nM). |
| In vitro | 在体外，saxagliptin可抑制FBS、胰岛素和IGF1诱导的间充质干细胞和MC3T3E1前成骨细胞的ERK磷酸化和细胞增殖。在没有生长因子的情况下，saxagliptin对ERK活化或细胞增殖没有影响。在间充质干细胞和 MC3T3E1 细胞中，有 FBS 存在时saxagliptin可抑制 Runx2 和骨钙素的表达、1 型胶原的生成和矿化，增加 PPAR-gamma 的表达[4]。 |
| In vivo | Saxagliptin hydrate 通过增加氮氧化物的供应和改善抗氧化状态，对2型糖尿病动物模型的动脉壁产生直接的有益影响。Saxagliptin hydrate 通过抑制 NAD(P)H 氧化酶驱动的 eNOS 解偶联，通过减少环氧合酶-1 衍生的血管收缩剂的作用和下调血栓素-类固醇受体的表达，逆转了 db/db 小鼠小动脉的血管肥厚重塑，并改善了 NO 的可用性[2]。Saxagliptin hydrate 抑制 DPP-4 还能改善餐后和空腹状态下的胰腺 β 细胞功能，降低餐后胰高血糖素浓度[3]。 |
| Cell experiments | Sub-confluent cells are serum-starved overnight and then incubated with 1.5 or 15 μM saxagliptin and/or FBS (1%), insulin (5 ng/mL) or IGF1 (10-8 M) for 24 h (effects on cell proliferation) or 1 h (effects on signal transduction mechanisms). (Only for Reference) |
| Target activity | DPP4:26 nM |
| Synonyms | 沙格列汀单水化合物, Onglyza hydrate, BMS-477118 hydrate |
| molecular weight | 333.43 |
| Molecular formula | C18H25N3O2·H2O |
| CAS | 945667-22-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 70 mg/mL (209.94 mM), Sonication is recommended. H2O: 1 mg/mL (3 mM) Ethanol: 61 mg/mL (182.9 mM) |
| References | 1. Neumiller JJ, et al. Am J Health Syst Pharm. 2010, 67(18):1515-25. 2. Solini A, et al. Vascul Pharmacol. 2016, 76:62-71. 3. Henry RR, et al. Diabetes Obes Metab. 2011, 13(9):850-8. 4. Sbaraglini ML, et al. Eur J Pharmacol. 2014, 727:8-14. |