Mosapride

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

Mosapride Chemical Structure

Mosapride Chemical Structure

CAS No. 112885-41-3

Purity & Quality Control

Batch: S483901 DMSO]84 mg/mL]false]]]false]]]false Purity: 98%
98

Mosapride Related Products

Biological Activity

Description Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist.
Targets
5HT4 [1]
In vitro
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
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].
Animal Research Animal Models Male Hartley guinea pigs
Dosages 3, 10 and 30 mg/kg
Administration i.g.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02056405 Unknown status
Postoperative Ileus
Hospital Italiano de Buenos Aires
December 2015 Phase 4
NCT02106130 Completed
Healthy
IlDong Pharmaceutical Co Ltd
May 2013 Phase 1
NCT01284764 Completed
Foreign Body Left During Endoscopic Examination
Inje University
January 2011 Phase 3
NCT01094847 Completed
Bioequivalence
Daewoong Pharmaceutical Co. LTD.
April 2010 Phase 1

Chemical Information & Solubility

Molecular Weight 421.89 Formula

C21H25ClFN3O3

CAS No. 112885-41-3 SDF --
Smiles CCOC1=CC(=C(C=C1C(=O)NCC2CN(CCO2)CC3=CC=C(C=C3)F)Cl)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 84 mg/mL ( (199.1 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)


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In vivo
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In vivo Formulation Calculator

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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.

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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.

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