Prucalopride
Based on 4 publication(s) in Google Scholar
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.
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- Reinheit: 99.93%
- CAS. Nr.: 179474-81-8
- Formel: C18H26ClN3O3
- Molecular Weight:367.87
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Prucalopride
MoreAlle 5-HT Receptor Isoform-spezifische Produkte anzeigen
More
Biologische Aktivität
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5-HT4A Receptor 8.6 (pKi) |
5-HT4B Receptor 8.1 (pKi) |
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Cell Line
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Type | Value | Description | References |
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| CHO | EC50 |
5.2 nM
Compound: Prucalopride
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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
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[PMID: 26363507] |
| HEK293 | EC50 |
26 nM
Compound: Prucalopride
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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
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[PMID: 26363507] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 cells
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Concentration:10 µM
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Incubation Time:24, 48, 72 h
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Result:Repressed lung cancer cells proliferation.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague dawley rats (diabetes mellitus (DM) model)[2].
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Dosage:5 or 10 µg/kg
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Administration:Oral gavage; single daily for 2 weeks.
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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).
Chemical Information
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CAS. Nr. 179474-81-8
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Appearance Solid
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Molecular Weight 367.87
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Formel C18H26ClN3O3
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Color White to off-white
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SMILES
ClC1=C(N)C(CCO2)=C2C(C(NC3CCN(CCCOC)CC3)=O)=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Nature
2023 Dec;624(7992):672-681. PMID: 37935376 -
Biochem Biophys Res Commun
Protective effects of prucalopride in MPTP-induced Parkinson's disease mice: Neurochemistry, motor function and gut barrier. [Abstract]2021 Jun 4:556:16-22. PMID: 33836343 -
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Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (271.84 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 50 mg/mL (135.92 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (135.92 mM); Clear solution; Need ultrasonic
Reinheit & Dokumentation
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Data Sheet (275 KB)
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SDS (563 KB)
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- Español - ES (563 KB)
- Swedish - SV (563 KB)
- Italian - IT (563 KB)
- Portuguese - PT (563 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Chen M, et al. Prucalopride inhibits lung cancer cell proliferation, invasion, and migration through blocking of the PI3K/AKT/mTor signaling pathway. Hum Exp Toxicol. 2020 Feb;39(2):173-181. [Content Brief]
[2]. Wang Y, et al. Prucalopride might improve intestinal motility by promoting the regeneration of the enteric nervous system in diabetic rats. Int J Mol Med. 2022 Jul;50(1):87. [Content Brief]
[3]. Briejer MR, et al. The in vitro pharmacological profile of prucalopride, a novel enterokinetic compound. Eur J Pharmacol. 2001 Jun 29;423(1):71-83. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 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 | |
| 100 mM | 0.0272 mL | 0.1359 mL | 0.2718 mL | 0.6796 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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