Cat. No.: HY-14149

Cisapride

(Synonyms: R 51619; (±)-Cisaprid)

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

Cisapride (R 51619) is an orally active 5-HT₄ receptor agonist with an EC₅₀ value of 140 nM. Cisapride is a hERG blocker with an IC₅₀ value of 9.4 nM. Cisapride is a gastroprokinetic agent that stimulates gastrointestinal motor activity.

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Pureté: 99.87%
CAS No.: 81098-60-4
Formule: C₂₃H₂₉ClFN₃O₄
Masse moléculaire:465.95

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Cisapride Chemical Structure

CAS No.: 81098-60-4

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (2)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

5-HT₄ Receptor

0.14 μM (EC₅₀)

Voir tous les produits spécifiques à Isoform 5-HT Receptor :

In Vitro

Cisapride (1-100 nM) is a potent hERG blockers with an IC₅₀ value of 9.4 nM^[1].
Cisapride (1-100 nM) shows efficacy to 5-HT₄ receptor with an EC₅₀ value of 140 nM^[1].
Cisapride (0.3, 1, 3, 10 and 30 μM) dose-dependently inhibits Kv4.3 with an IC₅₀ value of 9.8 μM in Kv4.3 potassium channels expressing CHO cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Cisapride (0.1-1 mg/kg; i.v., once) stimulates antral and colonic motility in conscious dogs^[3].
Cisapride (2 mg/kg (i.p.); 4 mg/kg, (oral administration); once) shows no significant differences in macroscopic features, histopathological features, cytokines profile and bodyweight changes with TNBS-treated rats^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male Wistar rats with trinitrobenzenesulfonic-acid-(TNBS) induced rat colitis^[4]
Dosage:

2 mg/kg (i.p.); 4 mg/kg, (oral administration)
Administration:

2 mg/kg, intraperitoneal injection ; 4 mg/kg, oral administration; once
Result:

Showed severe and intense transmural inflammation and diffuse necrosis, inflammatory granulomas and submucosal neutrophils infiltration in colitis rat. Induced body weight loss.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 81098-60-4
Appearance Solid
Masse moléculaire 465.95
Formule C₂₃H₂₉ClFN₃O₄
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
Synonyms

R 51619; (±)-Cisaprid
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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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ACS Omega

Computational Approaches to Identify Molecules Binding to Mycobacterium tuberculosis KasA. [Abstract]

2020 Nov 15;5(46):29935-29942. PMID: 33251429
Patent

US20260000674A1.

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1462 mL

10.7308 mL

21.4615 mL

5 mM

0.4292 mL

2.1462 mL

4.2923 mL

10 mM

0.2146 mL

1.0731 mL

2.1462 mL

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.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.37 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (277 KB)
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)
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)
Instruction de manipulation (2659 KB)

Références

[1]. Toga, T., Y. Kohmura, and R. Kawatsu, 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. 105(2): p. 207-10. [Content Brief]

[2]. Sung, K.W. and S.J. Hahn, Effect of mosapride on Kv4.3 potassium channels expressed in CHO cells. Naunyn Schmiedebergs Arch Pharmacol, 2013. 386(10): p. 905-16. [Content Brief]

[3]. Mine, Y, et al. Comparison of effect of mosapride citrate and existing 5-HT4 receptor agonists on gastrointestinal motility in vivo and in vitro. J Pharmacol Exp Ther, 1997. 283(3): p. 1000-8. [Content Brief]

[4]. Motavallian, A, et al., Does Cisapride, as a 5HT(4) Receptor Agonist, Aggravate the Severity of TNBS-Induced Colitis in Rat. Gastroenterol Res Pract, 2012. 2012: p. 362536. [Content Brief]

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.

Complete Stock Solution Preparation Table

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
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

Keywords

Cisapride

2 Cited Publications

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Cisapride

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Publications Citing Use of MedChemExpress (MCE) Cisapride

Voir tous les produits spécifiques à Isoform 5-HT Receptor

Activité biologique

Chemical Information

Publications (2)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Cisapride Related Classifications

HY-14149 Related Classifications