Cisapride hydrate

Catalog No.S4751 Synonyms: Propulsid, Alimix, Propulsin, Enteropride, Kinestase

Cisapride hydrate Chemical Structure

Molecular Weight(MW): 483.96

Cisapride acts directly as a selective serotonin 5-HT4 receptor agonist with IC50 of 0.483 μM. And It also acts indirectly as a parasympathomimetic.

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Biological Activity

Description Cisapride 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].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF7 cells NEfId|ZHfW6ldHnvckBie3OjeR?= NEXxT29KdmirYnn0bY9vKG:oIHj1cYFvKEWURzDpckBOS0Z5IHPlcIx{NCCLQ{WwQVAvODB4NE[g{txO M2HrVFE6OTFyM{Sx
HEK293 cells NFXU[GxHfW6ldHnvckBie3OjeR?= MVLJcohq[mm2aX;uJI9nKGi3bXHuJGVTTyC2ZGv3eFpHPjV4QW2gcZV1[W62IHX4dJJme3OnZDDpckBJTUt{OUOgZ4VtdHNiYomge4hwdGViY3XscEBx[XSlaDDjcIFueCCvZYToc4QtKEmFNUC9NE4xOSEQvF2= NVqzbWFiOTl{NkC3N|Q>
CHO cells NIrod2ZHfW6ldHnvckBie3OjeR?= NVziVJNyUW6qaXLpeIlwdiCxZjDoeY1idiCHUleg[ZhxemW|c3XkJIlvKEOKTzDj[YxteyCkeTD3bI9t\SClZXzsJJBifGOqIHPsZY1xKHSnY3jubZF2\SxiSVO1NF0xNjB|OUixJO69VQ>? M1zMe|E5PDR6M{Sy

... Click to View More Cell Line Experimental Data

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 T1/2 for cisapride is 1.48 h[1].

Protocol

Cell Research:[3]
+ Expand
  • 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.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Male Sprague-Dawley rats
  • Formulation: --
  • Dosages: 5 mg/kg
  • Administration: i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 96 mg/mL (198.36 mM)
Water Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 483.96
Formula

C23H29ClFN3O4.H2O

CAS No. 260779-88-2
Storage powder
in solvent
Synonyms Propulsid, Alimix, Propulsin, Enteropride, Kinestase

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01281553 Terminated Gastroesophageal Reflux Johnson & Johnson Pharmaceutical Research & Development L.L.C. September 2003 Phase 4
NCT01281553 Terminated Gastroesophageal Reflux Johnson & Johnson Pharmaceutical Research & Development L.L.C. September 2003 Phase 4
NCT01286090 Terminated Gastroparesis|Diabetes Mellitus Johnson & Johnson Pharmaceutical Research & Development L.L.C. July 2003 Phase 4
NCT01286090 Terminated Gastroparesis|Diabetes Mellitus Johnson & Johnson Pharmaceutical Research & Development L.L.C. July 2003 Phase 4
NCT01281540 Terminated Gastroparesis Johnson & Johnson Pharmaceutical Research & Development L.L.C. May 2003 Phase 4
NCT01281540 Terminated Gastroparesis Johnson & Johnson Pharmaceutical Research & Development L.L.C. May 2003 Phase 4

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID