1. Metabolic Enzyme/Protease
  2. Dipeptidyl Peptidase
  3. Saxagliptin hydrate

Saxagliptin hydrate (Synonyms: BMS-477118 hydrate)

目录号: HY-10285A
产品使用指南

Saxagliptin hydrate (BMS-477118 hydrate) 是一种有效,选择性,可逆,竞争性和具有口服活性的二肽基肽酶 4 (DPP-4) (Ki = 0.6-1.3 nM) 抑制剂。Saxagliptin hydrate 可用于 2 型糖尿病的研究。

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Saxagliptin hydrate Chemical Structure

Saxagliptin hydrate Chemical Structure

CAS No. : 945667-22-1

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Saxagliptin hydrate 的其他形式现货产品:

Other Forms of Saxagliptin hydrate:

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  • 生物活性

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  • 参考文献

生物活性

Saxagliptin hydrate (BMS-477118 hydrate) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin hydrate has the peotential for type 2 diabetes mellitus research[1][2][3].

IC50 & Target

Ki: 0.6-1.3 nM (Dipeptidyl peptidase-4 (DPP-4))[2]

体外研究
(In Vitro)

Saxagliptin (100 nM; 48 hours; INS-1 832/13 cells) treatment significantly induceS β-cell proliferation[1].
Saxagliptin (100 nM; 48 hours; INS-1 832/13 cells) treatment increases the p-AKT and active β-catenin protein levels, paralleled with the increase of c-myc and cyclin D1 protein expression[1].
Saxagliptin acts by preventing the degradation of glucagon-like peptide-1 and hence increases secretion of insulin and decreases secretion of glucagon[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: INS-1 832/13 cells
Concentration: 100 nM
Incubation Time: 48 hours
Result: Significantly induced β-cell proliferation.

Western Blot Analysis[1]

Cell Line: INS-1 832/13 cells
Concentration: 100 nM
Incubation Time: 48 hours
Result: Increased the p-AKT and active β-catenin protein levels, paralleled with the increase of c-myc and cyclin D1 protein expression.
体内研究
(In Vivo)

Saxagliptin (1 mg/kg; for 12 weeks) treatment in high-fat diet/streptozotocin-induced diabetic rats, significant improvement in pancreas insulin secretion capacity evaluated by hyperglycemia clamp and increased β-cell to α-cell areas ratio are observed[1].
Saxagliptin dose-dependently inhibits plasma DPP-4 activity in Han-Wistar rats, by ~70% at 7 hours postdose with 1 mg/kg and by ~90% at 7 hours postdose with 10 mg/kg. At 24 hours postdose, ~20% and 70% inhibition, respectively, remained[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
分子量

333.43

Formula

C18H27N3O3

CAS 号
中文名称

沙格列汀水合物;沙克列汀水合物

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
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  • 稀释计算器

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× = ×
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HY-10285A
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