Mosapride

Catalog No.S4839

For research use only.

Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist.

Mosapride Chemical Structure

CAS No. 112885-41-3

Purity & Quality Control

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Biological Activity

Description Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist.
Targets
5HT4 [1]
()
In vitro

Mosapride facilitates acetylcholine release from the enteric cholinergic neurons. It does not block K+ channels or D2 dopaminergic receptors[2]. Mosapride is a selective 5-HT4 receptor agonist with no affinity for 5-HT1, 5-HT2, adrenalineα1, adrenalineα2 or dopamine D2 receptors[3].

In vivo Mosapride augmented lower gastrointestinal motility in animal models and in patients with lower gastrointestinal disorders. It enhanced defecation responses in animal models. In human, after oral administration of single doses of mosapride 5-40 mg, peak mosapride concentrations (Cmax) were reached after about 1 hour. Both the Cmax and area under the concentration-time curve from time zero to infinity (AUC∞) increased in a dose-proportional manner. There were no significant differences in the pharmacokinetic profiles of mosapride administered as single or multiple doses. Mosapride is excreted in the urine and faeces. It is primarily metabolized in the liver by cytochrome P450 3A4 to the active metabolite, a des-4-fluorobenzyl compound[3].

Protocol (from reference)

Animal Research:

[1]

  • Animal Models: Male Hartley guinea pigs
  • Dosages: 3, 10 and 30 mg/kg
  • Administration: i.g.

Solubility (25°C)

In vitro

DMSO 84 mg/mL
(199.1 mM)


Chemical Information

Molecular Weight 421.89
Formula

C21H25ClFN3O3

CAS No. 112885-41-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCOC1=CC(=C(C=C1C(=O)NCC2CN(CCO2)CC3=CC=C(C=C3)F)Cl)N

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02056405 Unknown status Drug: Mosapride|Drug: Placebo Postoperative Ileus Hospital Italiano de Buenos Aires December 2015 Phase 4
NCT02106130 Completed Drug: Rebamipide|Drug: Mosapride citrate Healthy IlDong Pharmaceutical Co Ltd May 2013 Phase 1
NCT01284764 Completed Drug: Mosapride Foreign Body Left During Endoscopic Examination Inje University January 2011 Phase 3
NCT01094847 Completed Drug: DWJ1252 Bioequivalence Daewoong Pharmaceutical Co. LTD. April 2010 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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