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

Saxagliptin hydrochloride  (Synonyms: BMS-477118 hydrochloride)

目录号: HY-16448 纯度: 99.71%
COA 产品使用指南

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

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Saxagliptin hydrochloride Chemical Structure

Saxagliptin hydrochloride Chemical Structure

CAS No. : 709031-78-7

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5 mg ¥350
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10 mg ¥525
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25 mg ¥980
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50 mg ¥1540
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100 mg ¥2310
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Customer Review

Other Forms of Saxagliptin hydrochloride:

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 hydrochloride (BMS-477118 hydrochloride) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin hydrochloride 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 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

351.87

Formula

C18H26ClN3O2

CAS 号
性状

固体

颜色

White to off-white

中文名称

盐酸沙格列汀;盐酸沙克列汀

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 125 mg/mL (355.24 mM; 超声助溶; 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 : 100 mg/mL (284.20 mM; 超声助溶)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.8420 mL 14.2098 mL 28.4196 mL
5 mM 0.5684 mL 2.8420 mL 5.6839 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 (sealed storage, away from moisture and light)。-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

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
该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料
参考文献

Saxagliptin hydrochloride 相关分类

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 (sealed storage, away from moisture and light)。-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 2.8420 mL 14.2098 mL 28.4196 mL 71.0490 mL
5 mM 0.5684 mL 2.8420 mL 5.6839 mL 14.2098 mL
10 mM 0.2842 mL 1.4210 mL 2.8420 mL 7.1049 mL
15 mM 0.1895 mL 0.9473 mL 1.8946 mL 4.7366 mL
20 mM 0.1421 mL 0.7105 mL 1.4210 mL 3.5524 mL
25 mM 0.1137 mL 0.5684 mL 1.1368 mL 2.8420 mL
30 mM 0.0947 mL 0.4737 mL 0.9473 mL 2.3683 mL
40 mM 0.0710 mL 0.3552 mL 0.7105 mL 1.7762 mL
50 mM 0.0568 mL 0.2842 mL 0.5684 mL 1.4210 mL
60 mM 0.0474 mL 0.2368 mL 0.4737 mL 1.1841 mL
80 mM 0.0355 mL 0.1776 mL 0.3552 mL 0.8881 mL
100 mM 0.0284 mL 0.1421 mL 0.2842 mL 0.7105 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 hydrochloride
目录号:
HY-16448
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