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

Saxagliptin  (Synonyms: 沙格列汀; BMS-477118)

目录号: HY-10285 纯度: 99.96%
COA 产品使用指南

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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Saxagliptin Chemical Structure

Saxagliptin Chemical Structure

CAS No. : 361442-04-8

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     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥550
In-stock
1 mg ¥250
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5 mg ¥500
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10 mg ¥750
In-stock
25 mg ¥1400
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50 mg ¥2200
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100 mg ¥3400
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Other Forms of Saxagliptin:

查看 Dipeptidyl Peptidase 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1][2][3].

IC50 & Target

DPP-4

 

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 Viability 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

315.41

Formula

C18H25N3O2

CAS 号
性状

固体

颜色

White to off-white

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 中的溶解度 : ≥ 34 mg/mL (107.80 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

H2O 中的溶解度 : 10 mg/mL (31.70 mM; 超声助溶)

* "≥" 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
查看完整储备液配制表

* 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。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

In Vivo:

以下溶解方案,请直接配置工作液。建议现用现配,在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比; 如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶。

  • 方案 一

    请依序添加每种溶剂: PBS

    Solubility: 8.33 mg/mL (26.41 mM); 澄清溶液; 超声助溶 (<60°C)

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.96%

参考文献

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 3.1705 mL 15.8524 mL 31.7048 mL 79.2619 mL
5 mM 0.6341 mL 3.1705 mL 6.3410 mL 15.8524 mL
10 mM 0.3170 mL 1.5852 mL 3.1705 mL 7.9262 mL
15 mM 0.2114 mL 1.0568 mL 2.1137 mL 5.2841 mL
20 mM 0.1585 mL 0.7926 mL 1.5852 mL 3.9631 mL
25 mM 0.1268 mL 0.6341 mL 1.2682 mL 3.1705 mL
30 mM 0.1057 mL 0.5284 mL 1.0568 mL 2.6421 mL
DMSO 40 mM 0.0793 mL 0.3963 mL 0.7926 mL 1.9815 mL
50 mM 0.0634 mL 0.3170 mL 0.6341 mL 1.5852 mL
60 mM 0.0528 mL 0.2642 mL 0.5284 mL 1.3210 mL
80 mM 0.0396 mL 0.1982 mL 0.3963 mL 0.9908 mL
100 mM 0.0317 mL 0.1585 mL 0.3170 mL 0.7926 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Saxagliptin
目录号:
HY-10285
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