产品说明书
Saxagliptin hydrate
 |
同义名 : | 沙格列汀单水化合物 ;BMS-477118 hydrate;Onglyza hydrate |
| CAS号 : | 945667-22-1 | |
| 货号 : | A419052 | |
| 分子式 : | C18H27N3O3 | |
| 纯度 : | 99% | |
| 分子量 : | 333.425 | |
| MDL号 : | MFCD26131254 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Dipeptidylpeptidase 4 (DPP4) belongs to the S9b gene family of postproline serine peptidases. It acts mostly as a secreted membrane protein, mediating the degradation and inactivation of glucagon-like peptide (GLP)-1 and gastric inhibitory protein (GIP)[3]. Saxagliptin is a selective, reversible inhibitor of dipeptidyl peptidase-4 (DPP-4) approved for the treatment of type 2 diabetes mellitus in adults[4]. Treatment with 15 μM saxagliptin completely abolished the phosphorylation of extracellular-regulated kinase (ERK) induced by fetal bovine serum (FBS), insulin and IGF1. Saxagliptin (1.5 or 15 μM) inhibited type 1 collagen production after 14 days and decreased the formation of nodules of mineralization after 21 days[5]. Saxagliptin 2.5-400 mg daily resulted in measurable intact postprandial plasma GLP-1 concentrations that were 1.5-fold to 3-fold higher than those measured in patients receiving placebo. It also resulted in increased β-cell responsiveness to glucose in both the postprandial and fasting states, increased levels of intact GLP-1 and GIP after oral glucose administration, and decreased postprandial glucagon secretion[4]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
3.00mL 0.60mL 0.30mL |
15.00mL 3.00mL 1.50mL |
29.99mL 6.00mL 3.00mL |
| 参考文献 |
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