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Prucalopride Succinate 5-HT Receptor agonist

Name: Prucalopride Succinate
Brand: Selleck Chemicals
SKU: S4247
Availability: InStock
Rating: 5 (4 reviews)

Cat.No.S4247

Prucalopride(R-108512) is a selective, high affinity 5-HT4 receptor agonist. The Ki values of prucalopride for human 5-HT(4a) and 5-HT(4b) receptor are 2.5 nM and 8 nM, respectively.

Chemical Structure

Molecular Weight: 485.96

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Quality Control

Batch: Purity: 99.89%

99.89

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

Solubility

In vitro
Batch:

DMSO : 97 mg/mL (199.6 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 97 mg/mL

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.
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)

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Average weight of animals: g

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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	485.96	Formula	C₁₈H₂₆ClN₃O₃.C₄H₆O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	179474-85-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	R-108512			Smiles	COCCCN1CCC(CC1)NC(=O)C2=CC(=C(C3=C2OCC3)N)Cl.C(CC(=O)O)C(=O)O

Mechanism of Action

Targets/IC₅₀/Ki	5-HT4A 2.5 nM(Ki) 5-HT4B 8 nM(Ki)
In vitro	Prucalopride induces contractions in a concentration-dependent manner with pEC50 of 7.5. Prucalopride (1 mM) significantly amplifies the rebound contraction of the guinea-pig proximal colon after electrical field stimulation. Prucalopride induces relaxation of the rat oesophagus preparation of rat oesophagus tunica muscularis mucosae with pEC50 of 7.8, yielding a monophasic concentration–response curve. Prucalopride (0.1 μM) concentration-dependently increases the amplitude of submaximal cholinergic contractions and of acetylcholine release induced by electrical field stimulation in pig gastric circular muscle, and the effect is induced and enhanced IBMX (10 μM). Prucalopride (1 μM) significantly enhances the electrically induced cholinergic contractions in pig descending colon, and the facilitating effect is significantly enhanced by Rolipram.
In vivo	Prucalopride alters colonic contractile motility patterns in a dose-dependent fashion by stimulating high-amplitude clustered contractions in the proximal colon and by inhibiting contractile activity in the distal colon of fasted dogs. Prucalopride also causes a dose-dependent decrease in the time to the first giant migrating contraction (GMC); at higher doses of prucalopride, the first GMC generally occurres within the first half-hour after treatment.
References	[1] https://pubmed.ncbi.nlm.nih.gov/11438309/ [2] https://pubmed.ncbi.nlm.nih.gov/22266217/ [3] https://pubmed.ncbi.nlm.nih.gov/23454061/ [4] https://pubmed.ncbi.nlm.nih.gov/11696108/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04838522	Recruiting	Chronic Constipation	Takeda\|UC San Diego Human Milk Research Biorepository	March 2 2022	--
NCT04429802	Completed	Gastrointestinal Motility Disorder\|Dyspepsia	Universitaire Ziekenhuizen KU Leuven	September 26 2013	Not Applicable
NCT01807000	Completed	Healthy	Shire\|Takeda	March 18 2013	Phase 1
NCT01692132	Withdrawn	Chronic Constipation	Janssen Pharmaceutica	February 2013	--
NCT03279341	Completed	Chronic Constipation	University Hospital Gasthuisberg	December 3 2012	Phase 4
NCT01117051	Terminated	Non-cancer Pain\|Opioid Induced Constipation	Shire\|Takeda	May 19 2010	Phase 3

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