| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Cisapride (formerly R51619; R 51619; R-51619; Kaudalit; Prepulsid; Kinestase; Pridesia; Presid; Propulsid) is a benzamide-based nonselective agonist of serotonin 5-HT4 receptor. It has been approved to increase motility in the upper gastrointestinal tract, including disorders related to impaired gastrointestinal motility, such as functional dyspepsia and gastroesophageal reflux disease. It also functions as a strong inhibitor of the hERG potassium channel.
| Targets |
5-HT4 receptor ( EC50 = 140 nM ); hERG channel ( IC50 = 9.4 nM )
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|---|---|
| ln Vitro |
Cisapride is an agonist of the 5-HT4 receptor and an hERG blocker[1]. It is frequently used to treat disorders of gastrointestinal motility, including gastroparesis, slow-transit constipation, and chronic intestinal pseudo-obstruction, or gastroesophageal reflux disease (GERD). Through its ability to stimulate intestinal acetylcholine release from muscarinic receptors, cisapride works to promote motility of the gastrointestinal tract. Cisapride blocks the current in ventricular myocytes' L-type Ca2+ channels and the Kv 4.3 channels that are consistently expressed in Chinese hamster ovary (CEO) cells. In a concentration-dependent manner, cisapride inhibited Kv channel current without affecting its ability to act as a selective agonist of the serotonin 5-HT4 receptor[2].
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| ln Vivo |
Cisapride (0.1-1 mg/kg; injection, once) stimulates antral and aqueous motility in conscious dogs [3]. Endpoints of cisapride (2 mg/kg, (ip); 4 mg/kg, (oral); once) versus trinitrobenzene sulfonic acid treatment endpoints in terms of macroscopic features, histopathological features, cytokine profiles, and body weight changes There is no significant difference [4]. Animal model: Rat colitis induced by trinitrobenzene sulfonic acid (TNBS) in male Wistar rats [4] Dosage: 2 mg/kg (intraperitoneal injection); 4 mg/kg (orally) Administration method: 2 mg/kg, intraperitoneal injection; 4 mg/kg, oral administration; Results: Colitis rats developed severe and intense transmural inflammation and diffuse necrosis, inflammatory granuloma and submucosal neutrophil infiltration. Cause weight loss.
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| Animal Protocol |
Male Wistar rats with trinitrobenzenesulfonic-acid-(TNBS) induced rat colitis
2 mg/kg (i.p.); 4 mg/kg, (oral administration) 2 mg/kg, intraperitoneal injection ; 4 mg/kg, oral administration; once |
| References |
| Molecular Formula |
C23H29CLFN3O4
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|---|---|
| Molecular Weight |
465.95
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| Exact Mass |
465.18
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| Elemental Analysis |
C, 59.29; H, 6.27; Cl, 7.61; F, 4.08; N, 9.02; O, 13.73
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| CAS # |
81098-60-4
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| Related CAS # |
Cisapride monohydrate; 260779-88-2
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| Appearance |
Solid powder
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| SMILES |
CO[C@H]1CN(CC[C@H]1NC(=O)C2=CC(=C(C=C2OC)N)Cl)CCCOC3=CC=C(C=C3)F
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| InChi Key |
DCSUBABJRXZOMT-IRLDBZIGSA-N
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| InChi Code |
InChI=1S/C23H29ClFN3O4/c1-30-21-13-19(26)18(24)12-17(21)23(29)27-20-8-10-28(14-22(20)31-2)9-3-11-32-16-6-4-15(25)5-7-16/h4-7,12-13,20,22H,3,8-11,14,26H2,1-2H3,(H,27,29)/t20-,22+/m1/s1
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| Chemical Name |
4-amino-5-chloro-N-[(3S,4R)-1-[3-(4-fluorophenoxy)propyl]-3-methoxypiperidin-4-yl]-2-methoxybenzamide
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| Synonyms |
R51619; R 51619; R-51619; Kaudalit; Prepulsid; Kinestase; Pridesia; Presid; Propulsid
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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 |
| 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) |
DMSO: 93~100 mg/mL (199.6~214.6 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.37 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.37 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1462 mL | 10.7308 mL | 21.4615 mL | |
| 5 mM | 0.4292 mL | 2.1462 mL | 4.2923 mL | |
| 10 mM | 0.2146 mL | 1.0731 mL | 2.1462 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 |
| NCT01281566 | Terminated | Drug: Placebo Drug: Cisapride |
Infant, Premature Infant, Newborn |
Johnson & Johnson Pharmaceutical Research & Development, L.L.C. |
March 2003 | Phase 4 |
| NCT01286090 | Terminated | Drug: Placebo Drug: Cisapride |
Gastroparesis Diabetes Mellitus |
Johnson & Johnson Pharmaceutical Research & Development, L.L.C. |
July 2003 | Phase 4 |
| NCT01281540 | Terminated | Drug: Placebo Drug: Cisapride |
Gastroparesis | Johnson & Johnson Pharmaceutical Research & Development, L.L.C. |
May 2003 | Phase 4 |
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