2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. Prucalopride

Prucalopride  (Synonyms: 普芦卡必利)

目录号: HY-14151 纯度: 99.81%
COA 产品使用指南

摩尔计算器

Prucalopride 是一种口服有效的，具有选择性和特异性的 5-HT 4 受体激动剂，对人 5-HT4a/4b 受体具有高亲和力，其 pKi 值分别为 8.6 和 8.1。Prucalopride 通过促进大鼠肠道神经系统的再生来改善肠道运动能力。Prucalopride 还能通过阻断 PI3K/AKT/mTor 信号通路发挥抗癌活性。Prucalopride 可用于慢性便秘相关的运动障碍，假性肠梗阻以及癌症的研究。

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Prucalopride Chemical Structure

Prucalopride Chemical Structure

CAS No. : 179474-81-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥413
In-stock
5 mg ￥375
In-stock
10 mg ￥600
In-stock
50 mg ￥960
In-stock
100 mg ￥1680
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Other Forms of Prucalopride:

Prucalopride 相关抗体

Top Publications Citing Use of Products

查看 5-HT Receptor 亚型特异性产品:

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5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Prucalopride is an orally active, selective and specific 5-HT 4 receptor agonist (high affinity), with pKis of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer[1][2][3].

IC50 & Target

5-HT4A Receptor

8.6 (pKi)

5-HT4B Receptor

8.1 (pKi)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO EC50
5.2 nM
Compound: Prucalopride
Agonist activity at human 5HT4e receptor expressed in CHO cells assessed as cAMP level after 4 hrs by luciferase reporter gene assay
Agonist activity at human 5HT4e receptor expressed in CHO cells assessed as cAMP level after 4 hrs by luciferase reporter gene assay
[PMID: 26363507]
HEK293 EC50
26 nM
Compound: Prucalopride
Agonist activity at rat 5HT4e receptor expressed in HEK293 cells assessed as cAMP level after 30 mins by HTRF assay
Agonist activity at rat 5HT4e receptor expressed in HEK293 cells assessed as cAMP level after 30 mins by HTRF assay
[PMID: 26363507]
体外研究
(In Vitro)

Prucalopride (10 µM; 24, 48, 72 h) shows anti proliferative activity in A549 cells[1].
Prucalopride induces autophagy and apoptosis, decreases the expression of the phosphorylated protein kinase B (AKT) and mammalian target of rapamycin (mTor) in A549/A427 cells[1].

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

Prucalopride 相关抗体:

Cell Proliferation Assay[1]

Cell Line: A549 cells
Concentration: 10 µM
Incubation Time: 24, 48, 72 h
Result: Repressed lung cancer cells proliferation.
体内研究
(In Vivo)

Prucalopride (5, 10 µg/kg; p.o.; single daily for 2 weeks) shortens the colonic transit time in DM model, promotes the regeneration of colonic neural stem cells and neurons[2].
Prucalopride (5, 10 µg/kg; p.o.; single daily for 2 weeks) promotes the differentiation of colonic neural stem cells, activates the expression of glial proteins and promotes the recovery of neuronal injury to a certain extent[2].

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

Animal Model: Sprague dawley rats (diabetes mellitus (DM) model)[2].
Dosage: 5 or 10 µg/kg
Administration: Oral gavage; single daily for 2 weeks.
Result: Accelerated colonic movement and shortened the colonic transit time, and markedly increased the expression levels of Ki67.
Increased expression of SOX10 in the columnar epithelial nuclei and enteraden (when at 5 µg/kg), and in the columnar epithelial cells, the nuclei of lamina propria cells and enteraden (when at 10 µg/kg).
Significantly increased Nestin expression, which concentrated in columnar epithelial cells and the mesenchyme. (Nestin:a marker of enteric neural stem cells in the ENS).
Clinical Trial
分子量

367.87

Formula

C18H26ClN3O3
CAS 号
性状

固体

颜色

White to off-white

中文名称

普芦卡必利；普卢卡必利
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验： 

H2O 中的溶解度 : 50 mg/mL (135.92 mM; 超声助溶)

DMSO 中的溶解度 : ≥ 31 mg/mL (84.27 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)

* "≥" 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 2.7184 mL 13.5918 mL 27.1835 mL
5 mM 0.5437 mL 2.7184 mL 5.4367 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

* 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

动物实验：

以下溶解方案，请直接配制工作液。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 (135.92 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
参考文献

Prucalopride 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 2.7184 mL 13.5918 mL 27.1835 mL 67.9588 mL
5 mM 0.5437 mL 2.7184 mL 5.4367 mL 13.5918 mL
10 mM 0.2718 mL 1.3592 mL 2.7184 mL 6.7959 mL
15 mM 0.1812 mL 0.9061 mL 1.8122 mL 4.5306 mL
20 mM 0.1359 mL 0.6796 mL 1.3592 mL 3.3979 mL
25 mM 0.1087 mL 0.5437 mL 1.0873 mL 2.7184 mL
30 mM 0.0906 mL 0.4531 mL 0.9061 mL 2.2653 mL
40 mM 0.0680 mL 0.3398 mL 0.6796 mL 1.6990 mL
50 mM 0.0544 mL 0.2718 mL 0.5437 mL 1.3592 mL
60 mM 0.0453 mL 0.2265 mL 0.4531 mL 1.1326 mL
80 mM 0.0340 mL 0.1699 mL 0.3398 mL 0.8495 mL
H2O 100 mM 0.0272 mL 0.1359 mL 0.2718 mL 0.6796 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:

Prucalopride179474-81-8普芦卡必利普卢卡必利5-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorLung cancerchronic constipationpseudo-intestinal obstructionA549A427Inhibitorinhibitorinhibit

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