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Prucalopride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Prucalopride图片
CAS NO:179474-81-8
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
普芦卡必利
产品介绍
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。
生物活性

Prucalopride is an orally active, selective and specific5-HT 4 receptoragonist (high affinity), withpKis of 8.6 and 8.1 for human5-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 thePI3K/AKT/mTorsignaling pathway. Prucalopride can be used in studies of chronic constipation, pseudo-intestinal obstruction andcancer[1][2][3].

IC50& Target

5-HT4AReceptor

8.6 (pKi)

5-HT4BReceptor

8.1 (pKi)

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].

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].

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

性状

Solid

Formula

C18H26ClN3O3

CAS 号

179474-81-8

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°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

H2O : 50 mg/mL(135.92 mM;Need ultrasonic)

DMSO : ≥ 31 mg/mL(84.27 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.7184 mL13.5918 mL27.1835 mL
5 mM0.5437 mL2.7184 mL5.4367 mL
10 mM0.2718 mL1.3592 mL2.7184 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 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

  • 1.

    请依序添加每种溶剂: PBS

    Solubility: 50 mg/mL (135.92 mM); Clear solution; Need ultrasonic

*以上所有助溶剂都可在本网站选购。