Cisapride hydrate

Catalog No.S4751 Batch:S475102

Technical Data

Formula	C₂₃H₂₉ClFN₃O₄.H₂O
Molecular Weight	483.96	CAS No.	260779-88-2
Solubility (25°C)*	In vitro	DMSO	97 mg/mL (200.42 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

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.

Targets

5-HT4 receptor ^[1] (Cell-free assay)	hERG ^[1] (Cell-free assay)
0.483 μM	<1 μM

In vitro

Cisapride inhibits vascular Kv current independently of serotonin 5-HT4-receptor activation^[2]. 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^[3].

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^[2]. In rat, the PK profile indicate the T_1/2 for cisapride is 1.48 h^[1].

Protocol (from reference)

Cell Assay:^{^[3]}	Cell lines The human gastric cancer SGC7901, AGS, MGC803 and MKN45 cell lines and human immortalized gastric epithelial GES cell line Concentrations 0, 12.5, 25, 50, 100 or 200 nM Incubation Time 1, 3, 5 and 7 day Method Cells in the logarithmic growth phase are harvested and seeded in 96-well plates. The cell number is diluted to 5000/well in 200 microliters of RPMI1640 medium. In vitro experiments are carried out on the gastric cancer cell lines and GES cell line, using an MTT proliferation assay. MTT stains live cells, and the optical density absorbance at 490nm wavelength correlates with the cell number. Cisapride is added to the cells at concentrations of 0, 12.5, 25, 50, 100 or 200 nM and equivalent volume of ethanol is added as control in order to eliminate the effects of solvent. Twenty microliters of MTT is added to each well of the cell culture 4 h before termination of the culture at 37˚C. One hundred and fifty microliters of dimethyl sulfoxide is added to each well at the end of the culture and the plate is agitated for 10 minutes. The absorbency at 490 nm is read by a BIOHIT BP800 plate reader. Growth curve is drawn according to MTT colorimetry. The inhibition rate is calculated.
Animal Study:^{^[1]}	Animal Models Male Sprague-Dawley rats Dosages 5 mg/kg Administration i.v.

Cell Assay:^{^[3]}

Cell lines
The human gastric cancer SGC7901, AGS, MGC803 and MKN45 cell lines and human immortalized gastric epithelial GES cell line
Concentrations
0, 12.5, 25, 50, 100 or 200 nM
Incubation Time
1, 3, 5 and 7 day
Method
Cells in the logarithmic growth phase are harvested and seeded in 96-well plates. The cell number is diluted to 5000/well in 200 microliters of RPMI1640 medium. In vitro experiments are carried out on the gastric cancer cell lines and GES cell line, using an MTT proliferation assay. MTT stains live cells, and the optical density absorbance at 490nm wavelength correlates with the cell number. Cisapride is added to the cells at concentrations of 0, 12.5, 25, 50, 100 or 200 nM and equivalent volume of ethanol is added as control in order to eliminate the effects of solvent. Twenty microliters of MTT is added to each well of the cell culture 4 h before termination of the culture at 37˚C. One hundred and fifty microliters of dimethyl sulfoxide is added to each well at the end of the culture and the plate is agitated for 10 minutes. The absorbency at 490 nm is read by a BIOHIT BP800 plate reader. Growth curve is drawn according to MTT colorimetry. The inhibition rate is calculated.

Animal Study:^{^[1]}

Animal Models
Male Sprague-Dawley rats
Dosages
5 mg/kg
Administration
i.v.

References

Selleck's Cisapride hydrate has been cited by 1 publication

Deep learning detects cardiotoxicity in a high-content screen with induced pluripotent stem cell-derived cardiomyocytes [ Elife, 2021, 10e68714]	PubMed: 34338636

Deep learning detects cardiotoxicity in a high-content screen with induced pluripotent stem cell-derived cardiomyocytes [ Elife, 2021, 10e68714]

PubMed: 34338636

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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