Cisapride
Based on 2 publication(s) in Google Scholar
Cisapride (R 51619) is an orally active, selective 5-HT4 receptor agonist with an EC50 of 140 nM. Cisapride also acts as an hERG potassium channel blocker with an IC50 of 9.4 nM. Cisapride exerts gastrointestinal prokinetic effects by activating 5-HT4 receptors, but it also blocks the hERG potassium channel responsible for the repolarization phase of cardiac action potentials, delaying repolarization and thus prolonging the action potential duration. Cisapride can be used in research related to gastrointestinal dysfunction, gastroesophageal reflux disease, functional dyspepsia, chronic gastritis, gastroparesis, ulcerative colitis and necrotizing enterocolitis.
For research use only. We do not sell to patients.
- Purity: 99.87%
- CAS No.: 81098-60-4
- Formula: C23H29ClFN3O4
- Molecular Weight:465.95
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Cisapride
MoreAll 5-HT Receptor Isoforms
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Biological Activity
Description
IC50 & Target
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5-HT4 Receptor 140 nM (EC50) |
In Vitro
Cisapride (R 51619) (0.3-30 μM; 500 ms) monohydrate inhibits Kv4.3 potassium channels stably expressed in Chinese hamster ovary cells in a concentration-dependent manner, with an IC50 of 9.8 μM, and accelerates current decay[3].
Cisapride (10 min) monohydrate potently inhibits hERG potassium currents in HEK293 cells stably expressing hERG channels, with an IC50 of 9.4 nM[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Cisapride monohydrate improves intestinal motor function, significantly reduces TNF-α expression in the intestinal mucosa, and alleviates the severity of necrotizing enterocolitis in a mouse model of necrotizing enterocolitis[1].
Cisapride (2-4 mg/kg; once daily; i.p. or p.o.; consecutive dosing for 6 days) monohydrate does not alter the severity of colonic injury in TNBS-induced colitis in male Wistar rats[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar rats (male, 200 g, TNBS-induced ulcerative colitis)[5]
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Dosage:2 mg/kg; 4 mg/kg
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Administration:i.p., once daily for 6 days; p.o., once daily for 6 days
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Result:Did not significantly affect the body weight loss and diarrheal status of the rats.
Did not significantly aggravate colonic inflammatory damage macroscopically or microscopically.
Did not significantly alter myeloperoxidase (MPO) activity or proinflammatory cytokine (TNF-α, IL-1β, IL-6) levels in the inflamed colons.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 81098-60-4
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Appearance Solid
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Molecular Weight 465.95
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Formula C23H29ClFN3O4
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Color White to off-white
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SMILES
ClC1=C(N)C=C(OC)C(C(N[C@H]2[C@@H](OC)CN(CCCOC3=CC=C(F)C=C3)CC2)=O)=C1
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Synonyms
R 51619; (±)-Cisaprid
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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ACS Omega
Computational Approaches to Identify Molecules Binding to Mycobacterium tuberculosis KasA. [Abstract]2020 Nov 15;5(46):29935-29942. PMID: 33251429 -
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (214.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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.
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.
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 (5.37 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.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (292 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[3]. Sung KW, et al. Effect of mosapride on Kv4.3 potassium channels expressed in CHO cells. Naunyn-Schmiedeberg's archives of pharmacology. 2013 Oct;386(10):905-16. [Content Brief]
[5]. Toga T, et al. The 5-HT(4) agonists cisapride, mosapride, and CJ-033466, a Novel potent compound, exhibit different human ether-a-go-go-related gene (hERG)-blocking activities. J Pharmacol Sci. 2007 Oct;105(2):207-10. [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 |
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| DMSO | 1 mM | 2.1462 mL | 10.7308 mL | 21.4615 mL | 53.6538 mL |
| 5 mM | 0.4292 mL | 2.1462 mL | 4.2923 mL | 10.7308 mL | |
| 10 mM | 0.2146 mL | 1.0731 mL | 2.1462 mL | 5.3654 mL | |
| 15 mM | 0.1431 mL | 0.7154 mL | 1.4308 mL | 3.5769 mL | |
| 20 mM | 0.1073 mL | 0.5365 mL | 1.0731 mL | 2.6827 mL | |
| 25 mM | 0.0858 mL | 0.4292 mL | 0.8585 mL | 2.1462 mL | |
| 30 mM | 0.0715 mL | 0.3577 mL | 0.7154 mL | 1.7885 mL | |
| 40 mM | 0.0537 mL | 0.2683 mL | 0.5365 mL | 1.3413 mL | |
| 50 mM | 0.0429 mL | 0.2146 mL | 0.4292 mL | 1.0731 mL | |
| 60 mM | 0.0358 mL | 0.1788 mL | 0.3577 mL | 0.8942 mL | |
| 80 mM | 0.0268 mL | 0.1341 mL | 0.2683 mL | 0.6707 mL | |
| 100 mM | 0.0215 mL | 0.1073 mL | 0.2146 mL | 0.5365 mL |
Cisapride Related Classifications
HY-14149 Related Classifications
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Keywords
- Cisapride
- 81098-60-4
- R 51619
- (±)-Cisaprid
- R51619
- R-51619
- 5-HT Receptor
- Potassium Channel
- 5-HT4 receptors
- Kv4.3 potassium channels
- hERG channel
- necrotizing enterocolitis
- Chinese hamster ovary cells
- TNBS-induced colitis
- cardiac arrhythmia
- atrial arrhythmias
- HEK293 cells
- gastrointestinal motility
- Inhibitor
- inhibitor
- inhibit