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CAS No.: 945667-22-1

Saxagliptin hydrate/沙格列汀水合物 Catalog No. CSN13800

Synonyms: BMS-477118 hydrate;BMS-477118;Saxagliptin

Saxagliptin, the monohydrate form of anhydrous saxagliptin, is a reversible and selective DPP4 inhibitor with IC50 of 26 nM. It is used for the treatment of type 2 diabetes.

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技术信息

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].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.9992 mL
- 14.9959 mL
- 29.9917 mL
- 5 mM
- 0.5998 mL
- 2.9992 mL
- 5.9983 mL
- 10 mM
- 0.2999 mL
- 1.4996 mL
- 2.9992 mL

技术信息

CAS号

945667-22-1

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H27N3O3

运输

蓝冰

分子量

333.43

别名

BMS-477118 hydrate;BMS-477118;Saxagliptin;brand name: Onglyza

溶解度

DMSO	66.0 mg/mL (197.9 mM)
Ethanol	66.0 mg/mL (197.9 mM)

动物实验配方

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Saxagliptin hydrate/沙格列汀水合物 Catalog No. CSN13800