Saxagliptin
产品说明书
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同义名 : | 沙克列汀 ;BMS-477118 |
| CAS号 : | 361442-04-8 | |
| 货号 : | A354223 | |
| 分子式 : | C18H25N3O2 | |
| 纯度 : | 98% | |
| 分子量 : | 315.41 | |
| MDL号 : | MFCD12756398 | |
| 存储条件： |
Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 35 mg/mL(110.97 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO H2O: 10 mg/mL(31.7 mM)，配合低频超声助溶 |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Saxagliptin is a dipeptidyl peptidase 4 (DPP-4) inhibitor. DPP-4 inhibition with saxagliptin did not increase or decrease the rate of ischemic events, though the rate of hospitalization for heart failure was increased[3]. Generally, saxagliptin has similar efficacy compared with most oral antidiabetic drugs and may be more effective than acarbose, while having a better safety profile than both acarbose and sulfonylureas[4]. Saxagliptin has a shorter half-life than the other dipeptidyl-peptidase IV inhibitors, so it might be a better choice among drugs in this class for nursing mothers[5]. Dipeptidyl peptidase 4 inhibitors may have a protective effect in diabetic nephropathy. Treatment with saxagliptin improved ACR, even in the normoalbuminuric range, without affecting EGFR[6]. | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活性说明 | 数据源 |
| Caco-2 cells | Function assay | Inhibition of human DPP4 expressed in Caco-2 cells, Ki=0.6 nM | 17034148 | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT01646320 | - | Completed | - | - | |
| NCT02377388 | Platelet Aggregation During Ac... 展开 >>ute Myocardial Infarction 收起 << | Phase 3 | Recruiting | December 2019 | Brazil ... 展开 >> Heart Institute(InCor)-Acute Coronary Care Unit Recruiting São Paulo, SP, Brazil, 01406000 Contact: Paulo R Genestreti, MD 55 11 2661-5058 paulo.gen@ig.com.br Principal Investigator: Jose C Nicolau, MD,PhD Sub-Investigator: Paulo R Genestreti, MD 收起 << |
| NCT01646320 | Type 2 Diabetes | Phase 3 | Completed | - | - |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
3.17mL 0.63mL 0.32mL |
15.85mL 3.17mL 1.59mL |
31.70mL 6.34mL 3.17mL |
| 参考文献 |
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