2. Metabolic Enzyme/Protease Autophagy
  3. Dipeptidyl Peptidase Autophagy
  4. Sitagliptin phosphate monohydrate

Sitagliptin phosphate monohydrate  (Synonyms: 西他列汀磷酸盐一水合物; MK-0431 phosphate monohydrate)

目录号: HY-13749B 纯度: 99.49%
COA 产品使用指南

摩尔计算器

Sitagliptin (MK0431 phosphate monohydrate) 是一种有效的 DPP4 抑制剂，在 Caco-2 细胞中，IC50 值为 19 nM。

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Sitagliptin phosphate monohydrate Chemical Structure

Sitagliptin phosphate monohydrate Chemical Structure

CAS No. : 654671-77-9

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规格 价格 是否有货 数量
10 mM * 1 mL in Water ￥528
In-stock
100 mg ￥480
In-stock
200 mg ￥680
In-stock
500 mg   询价  
1 g   询价  

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Customer Review

Other Forms of Sitagliptin phosphate monohydrate:

Sitagliptin phosphate monohydrate 相关抗体

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DPP-1 DPP-2 DPP-4 DPP-8 DPP-9

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Sitagliptin phosphate monohydrate (MK-0431 phosphate monohydrate) is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts[1].

IC50 & Target

IC50: 19 nM (DPP4, in Caco-2 cell extracts)
体外研究
(In Vitro)

Sitagliptin phosphate exhibits a potent inhibitory effect on DPP-4 with IC50 of 19 nM from Caco-2 cell extracts[1]. Sitagliptin reduces in vitro migration of isolated splenic CD4 T-cells through a pathway involving cAMP/PKA/Rac1 activation[2]. A recent study demonstrates that sitagliptin exerts a novel, direct action in order to stimulate GLP-1 secretion by the intestinal L cell through a DPP-4-independent, protein kinase A- and MEK-ERK1/2-dependent pathway. It therefore reduces the effect of autoimmunity on graft survival[3].

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

Sitagliptin phosphate monohydrate 相关抗体:
体内研究
(In Vivo)

In vivo, the ED50 value of sitagliptin phosphate for inhibition of plasma DPP-4 activity is calculated to be 2.3 mg/kg 7 hour postdose and 30 mg/kg 24 hour postdose in freely fed Han-Wistar rats[1]. The streptozotocin-induced type 1 diabetes mouse model exhibits elevated DPP-4 levels in the plasma that can be substantially inhibited in mice on an Sitagliptin phosphate diet. This is achieved by a positive effect on the regulation of hyperglycemia, potentially through prolongation of islet graft survival[4]. The plasma clearance and volume of distribution of Sitagliptin phosphate are higher in rats (40-48 mL/min/kg, 7-9 L/kg) than in dogs (9 mL/min/kg, 3 L/kg); and its half-life is shorter in rats,2 hours compared with 4 hours in dogs[5].

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

523.32

Formula

C16H20F6N5O6P
CAS 号
性状

固体

颜色

White to off-white

中文名称

磷酸西他列汀一水合物
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

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

溶解性数据
In Vitro: 

H2O 中的溶解度 : ≥ 33 mg/mL (63.06 mM)

* "≥" 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 1.9109 mL 9.5544 mL 19.1088 mL
5 mM 0.3822 mL 1.9109 mL 3.8218 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)。-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: 50 mg/mL (95.54 mM); 澄清溶液; 超声助溶

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

只
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

纯度: 99.49%

COA (175 KB) LCMS (269 KB)

产品使用指南 (1538 KB)
参考文献
Cell Assay
[2]

CD4T-cells are plated on membrane inserts in serum-free RPMI 1640, and cell migration is assayed using Transwell chambers (Corning), in the presence or absence of purified porcine kidney DPP-4 (32.1 units/mg; 100 mU/mL final concentration) and DPP-4 inhibitor (100 μM). After 1 hour, cells on the upper surface are removed mechanically, and cells that have migrated into the lower compartment are counted. The extent of migration is expressed relative to the control sample.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice: Overnight fasted C57BL/6J mice are challenged 45 min after compound administration with an oral glucose load (2 g/kg). Blood samples for glucose measurement are obtained by tail bleed predose and at serial time points after the glucose load. To evaluate the duration of the effect on glucose tolerance, vehicle or DPP-4 inhibitors are administered 16 h before the glucose challenge.

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

Sitagliptin phosphate monohydrate 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)。-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 1 mM 1.9109 mL 9.5544 mL 19.1088 mL 47.7719 mL
5 mM 0.3822 mL 1.9109 mL 3.8218 mL 9.5544 mL
10 mM 0.1911 mL 0.9554 mL 1.9109 mL 4.7772 mL
15 mM 0.1274 mL 0.6370 mL 1.2739 mL 3.1848 mL
20 mM 0.0955 mL 0.4777 mL 0.9554 mL 2.3886 mL
25 mM 0.0764 mL 0.3822 mL 0.7644 mL 1.9109 mL
30 mM 0.0637 mL 0.3185 mL 0.6370 mL 1.5924 mL
40 mM 0.0478 mL 0.2389 mL 0.4777 mL 1.1943 mL
50 mM 0.0382 mL 0.1911 mL 0.3822 mL 0.9554 mL
60 mM 0.0318 mL 0.1592 mL 0.3185 mL 0.7962 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.

Keywords:

Sitagliptin phosphate654671-77-9MK-0431 phosphate磷酸西他列汀一水合物Dipeptidyl PeptidaseAutophagyDPPInhibitorinhibitorinhibit

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