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Cat. No.: HY-14149A

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Cisapride monohydrate

Name: Cisapride monohydrate
Brand: MedChemExpress
SKU: HY-14149A
Price: 50.00 USD
Availability: InStock
Rating: 5 (2 reviews)

(Synonyms: R 51619 monohydrate; (±)-Cisaprid monohydrate)

2 Cited Publications

Customer Review

Based on 2 publication(s) in Google Scholar

Cisapride (R 51619) monohydrate is an orally active, selective 5-HT₄ receptor agonist with an EC₅₀ of 140 nM. Cisapride monohydrate also acts as an hERG potassium channel blocker with an IC₅₀ of 9.4 nM. Cisapride monohydrate 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 monohydrate 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.: 260779-88-2
Formula: C₂₃H₃₁ClFN₃O₅
Molecular Weight:483.96

Storage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Cisapride monohydrate Chemical Structure

CAS No.: 260779-88-2

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

IC₅₀ & Target

^[5]

5-HT₄ Receptor

140 nM (EC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC50	9.4 nM	Inhibition of human ether-a-go-go-related gene (hERG) potassium currents in HEK293 cells stably expressing hERG channels assessed via whole-cell patch-clamp electrophysiological assay with 10 min incubation. Inhibition of human ether-a-go-go-related gene (hERG) potassium currents in HEK293 cells stably expressing hERG channels assessed via whole-cell patch-clamp electrophysiological assay with 10 min incubation.	PMC3408677

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 (R 51619) monohydrate (1 mM; i.p.; single dose) exhibits activities of increasing heart rate and left ventricular ejection fraction in anesthetized transgenic mouse animal models^[2].
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.

Animal Model:

Wistar rats (male, 200 g, TNBS-induced ulcerative colitis)^[5]
Dosage:

2 mg/kg; 4 mg/kg
Administration:

i.p., once daily for 6 days; p.o., once daily for 6 days
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.

Chemical Information

CAS No. 260779-88-2
Appearance Solid
Molecular Weight 483.96
Formula C₂₃H₃₁ClFN₃O₅
Color White to off-white
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.O
Synonyms

R 51619 monohydrate; (±)-Cisaprid monohydrate
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (2)

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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
Patent

US20260000674A1.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (289 KB)
SDS (476 KB)
- English - EN (476 KB)
- Français - FR (476 KB)
- Deutsch - DE (476 KB)
- Norwegian - NO (476 KB)
- Español - ES (476 KB)
- Swedish - SV (476 KB)
- Italian - IT (476 KB)
- Korean - KR (476 KB)
- Portuguese - PT (476 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Kovler ML, et al. Toll-like receptor 4-mediated enteric glia loss is critical for the development of necrotizing enterocolitis. Science translational medicine. 2021 Sep 22;13(612):eabg3459.

[2]. Keller N, et al. Cardiovascular effects of cisapride and prucalopride on human 5-HT receptors in transgenic mice. Naunyn-Schmiedeberg's archives of pharmacology. 2018 Sep;391(9):975-985.

[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]

[4]. Motavallian, et al. Does Cisapride, as a 5HT4 Receptor Agonist, Aggravate the Severity of TNBS‐Induced Colitis in Rat?. Gastroenterology Research and Practice 2012.1 (2012): 362536.

[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]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Keywords

Cisapride monohydrate

2 Cited Publications

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Purity & Documentation
References

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Cisapride monohydrate

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