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Purity: ≥98%
Prucalopride (R 108512; R108512; R 108512; trade names: Resolor; Resotran; Motegrity), a novel enterokinetic and benzofuran-based compound, is a novel, selective, high affinity 5-HT (serotonin) receptor agonist for 5-HT4A and 5-HT4B receptor with anti-idiopathic constipation activity. It shows >290-fold selectivity for 5-HT4A and 5-HT4B over other 5-HT receptor subtypes and inhibits 5-HT4A and 5-HT4B with Ki values of 2.5 nM and 8 nM, respectively. With a pEC50 of 7.5, prucalopride causes contractions in a concentration-dependent manner. Following electrical field stimulation, prucalopride dramatically increases the guinea pig proximal colon's rebound contraction. The FDA approved prucalopride in December 2018 for the treatment of idiopathic chronic constipation.
| Targets |
5-HT4A Receptor ( pKi = 8.6 ); 5-HT4B Receptor ( pKi = 8.1 )
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| ln Vivo |
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| Animal Protocol |
In the prefrontal cortex, prucalopride maximally increased ACh and histamine levels at 5 and 10 mg/kg, while PRX-03140 significantly increased cortical histamine levels at 50 mg/kg, failing to affect ACh release at doses below 150 mg/kg, according to studies using microdialysis in rats.
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| References |
| Molecular Formula |
C22H32CLN3O7
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| Molecular Weight |
485.96
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| Exact Mass |
485.19
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| Elemental Analysis |
C, 54.38; H, 6.64; Cl, 7.29; N, 8.65; O, 23.05
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| CAS # |
179474-85-2
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| Related CAS # |
Prucalopride; 179474-81-8
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| Appearance |
Solid powder
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| SMILES |
COCCCN1CCC(CC1)NC(=O)C2=CC(=C(C3=C2OCC3)N)Cl.C(CC(=O)O)C(=O)O
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| InChi Key |
QZRSNVSQLGRAID-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H26ClN3O3.C4H6O4/c1-24-9-2-6-22-7-3-12(4-8-22)21-18(23)14-11-15(19)16(20)13-5-10-25-17(13)14;5-3(6)1-2-4(7)8/h11-12H,2-10,20H2,1H3,(H,21,23);1-2H2,(H,5,6)(H,7,8)
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| Chemical Name |
4-amino-5-chloro-N-[1-(3-methoxypropyl)piperidin-4-yl]-2,3-dihydro-1-benzofuran-7-carboxamide;butanedioic acid
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0578 mL | 10.2889 mL | 20.5778 mL | |
| 5 mM | 0.4116 mL | 2.0578 mL | 4.1156 mL | |
| 10 mM | 0.2058 mL | 1.0289 mL | 2.0578 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02047045 | Completed | Procedure: acupuncture Drug: Prucalopride |
Constipation | Guang'anmen Hospital of China Academy of Chinese Medical Sciences |
April 2014 | Not Applicable |
| NCT01870674 | Completed | Drug: YH12852 Drug: Prucalopride Drug: Placebo |
Healthy | Yuhan Corporation | August 2013 | Phase 1 |
| NCT03279341 | Completed | Drug: Prucalopride Drug: Bisacodyl Drug: polyethylene glycol |
Chronic Constipation | University Hospital, Gasthuisberg |
December 3, 2012 | Phase 4 |
| NCT05966246 | Completed | Drug: Arm I : Experimental (Prucalopride succinate group) Drug: Arm II : Control (Mosapride citrate group) |
Gastric Cancer | Gangnam Severance Hospital | January 25, 2022 | Not Applicable |
| NCT01807000 | Completed | Drug: Radiolabeled Prucalopride Succinate |
Healthy | Shire | March 18, 2013 | Phase 1 |
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