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) |
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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. |
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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). |
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| 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 | 6 months | | -20°C | 1 month |
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| 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 | 1 mM | 2.7184 mL | 13.5918 mL | 27.1835 mL | | 5 mM | 0.5437 mL | 2.7184 mL | 5.4367 mL | | 10 mM | 0.2718 mL | 1.3592 mL | 2.7184 mL |
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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。 |
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