Saxagliptin (Synonyms:沙格列汀; BMS-477118)
目录号 : KM2446 CAS No. : 361442-04-8 纯度 : 98%

Saxagliptin (BMS-477118) 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 可用于 2 型糖尿病的研究。

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10mg
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50mg
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100mg
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500mg 询价 In-stock

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生物活性

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

体外研究

Saxagliptin (100 nM; 48 hours; INS-1 832/13 cells) treatment significantly induceS β-cell proliferation.
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.
Saxagliptin acts by preventing the degradation of glucagon-like peptide-1 and hence increases secretion of insulin and decreases secretion of glucagon.

Cell Viability Assay

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

Western Blot Analysis

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

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.
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.

分子式
C18H25N3O2
分子量
315.41
CAS号
361442-04-8
中文名称
沙格列汀;沙克列汀
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

溶解性数据
In Vitro: 

DMSO : ≥ 34 mg/mL (107.80 mM)

H2O : 10 mg/mL (31.70 mM; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.1705 mL 15.8524 mL 31.7048 mL
5 mM 0.6341 mL 3.1705 mL 6.3410 mL
10 mM 0.3170 mL 1.5852 mL 3.1705 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

临床试验
科研文献
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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