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Cisapride hydrate 5-HT Receptor agonist

Name: Cisapride hydrate
Brand: Selleck Chemicals
SKU: S4751
Availability: InStock
Rating: 5 (2 reviews)

Cat.No.S4751

Cisapride (Propulsid, Alimix, Propulsin, Enteropride, Kinestase) acts directly as a selective serotonin 5-HT4 receptor agonist with IC50 of 0.483 μM. And It also acts indirectly as a parasympathomimetic.

Chemical Structure

Molecular Weight: 483.96

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Quality Control

Batch: Purity: 99.69%

99.69

Related Targets	Adrenergic Receptor AChR COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR
Other 5-HT Receptor Inhibitors	WAY-100635 Maleate Puerarin Serotonin (5-HT) HCl SB269970 HCl Ketanserin BRL-15572 Dihydrochloride Nuciferine RS-127445 Flopropione Azacyclonol

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Activity Description
MCF7 cells	Function assay	Inhibition of human ERG in MCF7 cells, IC50=0.00646 μM
HEK293 cells	Function assay	Inhibition of human ERG td[wt:F656A] mutant expressed in HEK293 cells by whole cell patch clamp method, IC50=0.01 μM
CHO cells	Function assay	Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique, IC50=0.03981 μM
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 96 mg/mL (198.36 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

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.

Chemical Information, Storage & Stability

Molecular Weight	483.96	Formula	C₂₃H₂₉ClFN₃O₄.H₂O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	260779-88-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Propulsid, Alimix, Propulsin, Enteropride, Kinestase			Smiles	COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F.O

Mechanism of Action

Targets/IC₅₀/Ki	5-HT4 receptor (Cell-free assay) 0.483 μM hERG (Cell-free assay) <1 μM
In vitro	Cisapride inhibits vascular Kv current independently of serotonin 5-HT4-receptor activation. As HERG channel blocker, cisapride, can inhibit the growth of gastric cancer cells by altering distribution of cell cycle and inducing apoptosis so as to be of potential value in the treatment of gastric cancer. Cisapride could inhibit the growth and clonogenicity of human gastric cancer lines by specific blockage of HERG channel in a time- and dose-dependent manner while has little effects on GES cells.
In vivo	Cisapride is widely prescribed for the treatment of gastrointestinal motility dysfunctions, such as gastroesophageal reflux disorder (GERD), chronic intestinal pseudo-obstruction, and slow-transit constipation gastroparesis. Although cisapride is a beneficial prokinetic agent, several common side effects, such as abdominal pain, nausea, diarrhea, and increased frequency of urination, have been reported. In rat, the PK profile indicate the T_1/2 for cisapride is 1.48 h.
References	[1] https://pubmed.ncbi.nlm.nih.gov/26761776/ [2] https://pubmed.ncbi.nlm.nih.gov/27569285/ [3] https://pubmed.ncbi.nlm.nih.gov/15846098/

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