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Cisapride (R 51619) 5-HT Receptor agonist

Name: Cisapride (R 51619)
Brand: Selleck Chemicals
SKU: S5253
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S5253

Cisapride (R 51619, Kaudalit, Kinestase, Prepulsid, Presid, Pridesia, Propulsid) is a nonselective 5-HT4 receptor agonist with gastroprokinetic effects.

Chemical Structure

Molecular Weight: 465.95

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.82%

99.82

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Chemical Information, Storage & Stability

Molecular Weight	465.95	Formula	C₂₃H₂₉ClFN₃O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	81098-60-4	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Kaudalit, Kinestase, Prepulsid, Presid, Pridesia, Propulsid			Smiles	COC1CN(CCC1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F

Solubility

In vitro
Batch:

DMSO : 93 mg/mL ( (199.59 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.65mg/ml (9.98mM)	Taking the 1 mL working solution as an example, add 50 μL of 93 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.66mg/ml (1.42mM)	Taking the 1 mL working solution as an example, add 50 μL of 13.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
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.

Mechanism of Action

Targets/IC₅₀/Ki	hERG channel ^[1] 9.4 nM 5-HT4 receptor ^[1] 140 nM(EC50)
In vitro	Cisapride (R 51619) is a 5-HT4 receptor agonist and also a hERG blocker^[1], widely used for the treatment of gastrointestinal motility dysfunctions such as gastroesophageal reflux disorder (GERD), chronic intestinal pseudo-obstruction, and slow-transit constipation gastroparesis. It works by promoting gastrointestinal motility through stimulating the release of intestinal acetylcholine from muscarinic receptors. This compound inhibits Kv 4.3 channels stably expressed in Chinese hamster ovary (CEO) cells as well as the current in L-type Ca2+ channels of ventricular myocytes. It inhibited Kv channel current in a concentration-dependent manner independent of its function as a selective serotonin 5-HT4-receptor agonist^[2].
References	https://www.tandfonline.com/doi/abs/10.1517/13543784.2010.482927 https://pubmed.ncbi.nlm.nih.gov/15846098/

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