Prucalopride succinate
Based on 4 publication(s) in Google Scholar
Prucalopride succinate 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 succinate improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride succinate also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride succinate can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer.
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- Pureza: 99.94%
- No. CAS: 179474-85-2
- Fòrmula: C22H32ClN3O7
- Peso molecular:485.96
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Prucalopride succinate
MoreVer todos los productos específicos de isoformas 5-HT Receptor
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Actividad biológica
Descripciòn
IC50 & Target
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5-HT4A Receptor 8.6 (pKi) |
5-HT4B Receptor 8.1 (pKi) |
In Vitro
Prucalopride succinate (10 µM; 24, 48, 72 h) shows anti proliferative activity in A549 cells[4].
Prucalopride succinate induces autophagy and apoptosis, decreases the expression of the phosphorylated protein kinase B (AKT) and mammalian target of rapamycin (mTor) in A549/A427 cells[4].
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.
In Vivo
Prucalopride succinate (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[3].
Prucalopride succinate (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[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Diabetes mellitus (DM) rat models[3]
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Dosage:5 μg/kg, 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).
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 179474-85-2
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Appearance Solid
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Peso molecular 485.96
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Fòrmula C22H32ClN3O7
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Color White to off-white
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SMILES
O=C(O)CCC(O)=O.O=C(C1=C(OCC2)C2=C(N)C(Cl)=C1)NC3CCN(CCCOC)CC3
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Synonyms
R-108512
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Solvente y solubilidad
In Vitro:
DMSO : 50 mg/mL (102.89 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 20 mg/mL (41.16 mM)
* "≥" means soluble, but saturation unknown.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- 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: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.14 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.14 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Pureza y Documentación
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Ficha de datos (280 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. 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]
[2]. Johnson DE, et al. The 5-hydroxytryptamine4 receptor agonists prucalopride and PRX-03140 increase acetylcholine and histamine levels in the rat prefrontal cortex and the power of stimulated hippocampal θ oscillations. J Pharmacol Exp Ther. 2012 Jun;341(3):681-91. [Content Brief]
[3]. 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]
[4]. 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]
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| H2O / DMSO | 1 mM | 2.0578 mL | 10.2889 mL | 20.5778 mL | 51.4446 mL |
| 5 mM | 0.4116 mL | 2.0578 mL | 4.1156 mL | 10.2889 mL | |
| 10 mM | 0.2058 mL | 1.0289 mL | 2.0578 mL | 5.1445 mL | |
| 15 mM | 0.1372 mL | 0.6859 mL | 1.3719 mL | 3.4296 mL | |
| 20 mM | 0.1029 mL | 0.5144 mL | 1.0289 mL | 2.5722 mL | |
| 25 mM | 0.0823 mL | 0.4116 mL | 0.8231 mL | 2.0578 mL | |
| 30 mM | 0.0686 mL | 0.3430 mL | 0.6859 mL | 1.7148 mL | |
| 40 mM | 0.0514 mL | 0.2572 mL | 0.5144 mL | 1.2861 mL | |
| DMSO | 50 mM | 0.0412 mL | 0.2058 mL | 0.4116 mL | 1.0289 mL |
| 60 mM | 0.0343 mL | 0.1715 mL | 0.3430 mL | 0.8574 mL | |
| 80 mM | 0.0257 mL | 0.1286 mL | 0.2572 mL | 0.6431 mL | |
| 100 mM | 0.0206 mL | 0.1029 mL | 0.2058 mL | 0.5144 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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