| Size | Price | Stock | Qty |
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| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
5-HT4 receptor (serotonin receptor 4 / HTR4). Revexepride is a highly selective agonist of the 5-HT4 receptor. Activation of 5-HT4 receptors in the gastrointestinal tract stimulates the release of acetylcholine and other neurotransmitters, enhancing gastrointestinal motility and accelerating gastric emptying. The compound's selectivity for the 5-HT4 receptor is a key feature of its prokinetic activity.
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| ln Vitro |
Revepride is metabolized by human CYP isoenzymes; in vitro, CYP3A4 metabolizes it most efficiently (99.9%), with CYP2D6 contributing less (0.1%). In vitro, revexepride directly inhibits human CYP3A4 with IC50 values ranging from 16 to 49 μM [1].
In vitro, Revexepride demonstrates high selectivity and potency as a 5-HT4 receptor agonist. The compound stimulates gastrointestinal motility in tissue-based assays using isolated intestinal segments. Its metabolism is primarily mediated by CYP3A4, which accounts for 99.9% of its in vitro metabolism. The compound's potential to induce CYP3A4 has been noted. |
| ln Vivo |
In vivo, Revexepride has been evaluated in animal models of gastrointestinal motility disorders. The compound stimulates gastrointestinal motility and accelerates gastric emptying, consistent with its mechanism as a 5-HT4 receptor agonist. Its prokinetic activity has been demonstrated in preclinical studies, supporting its potential for the treatment of GERD and gastroparesis. Clinical studies have been conducted to evaluate its efficacy and safety in patients.
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| Enzyme Assay |
Cell-free receptor binding assays for Revexepride use membrane preparations from cells expressing recombinant human 5-HT4 receptors. The compound is incubated with a radiolabeled 5-HT4 receptor ligand (e.g., [³H]-GR113808) at varying concentrations for 60-120 minutes at room temperature. Nonspecific binding is determined in the presence of an excess of unlabeled 5-HT4 receptor ligand. Bound and free radioactivity are separated by filtration, and Ki values are calculated from competition curves.
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| Cell Assay |
Cellular functional assays for Revexepride use cell lines stably expressing the 5-HT4 receptor (e.g., HEK-293-5-HT4 cells). Cells are seeded in 96-well plates and treated with Revexepride at concentrations ranging from 0.01 nM to 100 μM. Receptor activation is measured by monitoring cAMP accumulation via HTRF or ELISA-based cAMP assays, as 5-HT4 receptors are Gs-coupled and stimulate adenylyl cyclase. EC50 values are determined from dose-response curves. Selectivity is confirmed by testing the compound against other 5-HT receptor subtypes.
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| Animal Protocol |
In vivo efficacy studies are conducted in rodent models of delayed gastric emptying or gastrointestinal motility disorders. Revexepride is administered orally at doses typically ranging from 0.1-10 mg/kg. Gastric emptying is measured using a standard test meal containing a non-absorbable marker (e.g., charcoal or phenol red) or using scintigraphy with radiolabeled test meals. Gastrointestinal transit is assessed by measuring the distance traveled by a marker along the intestinal tract. Prokinetic activity is calculated from dose-response curves.
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| ADME/Pharmacokinetics |
Pharmacokinetic studies of Revexepride demonstrate that the compound is metabolized primarily by CYP3A4, which accounts for 99.9% of its in vitro metabolism. The compound's potential to induce CYP3A4 may have implications for drug-drug interactions. PK parameters such as Cmax, Tmax, AUC, half-life, and oral bioavailability are determined in preclinical species and in clinical studies. The compound's favorable PK properties support oral dosing for gastrointestinal disorders.
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| Toxicity/Toxicokinetics |
Toxicology studies of Revexepride were conducted as part of its clinical development program. As a 5-HT4 receptor agonist, potential toxicities may include cardiovascular effects (e.g., arrhythmias) and gastrointestinal effects. Standard toxicology studies (acute, subchronic, and chronic) were performed in rodents and non-human primates. The compound's safety profile was evaluated in clinical trials for GERD and gastroparesis. Specific toxicity findings are not widely reported in public sources.
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| References | |
| Additional Infomation |
Revexepride (SSP-002358) is a clinical-stage drug candidate for the treatment of gastroesophageal reflux disease (GERD) and gastroparesis. It was developed as a novel prokinetic agent with high selectivity for the 5-HT4 receptor. The compound has been evaluated in clinical trials, though its development status is not currently active. Revexepride is available for research purposes. Its mechanism as a 5-HT4 agonist makes it a valuable tool for studying gastrointestinal motility and developing treatments for motility disorders.
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| Molecular Formula |
C21H32CLN3O4
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|---|---|
| Molecular Weight |
425.954
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| Exact Mass |
425.208
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| Elemental Analysis |
C, 59.22; H, 7.57; Cl, 8.32; N, 9.87; O, 15.02
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| CAS # |
219984-49-3
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| PubChem CID |
9823762
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| Appearance |
White to yellow solid powder
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| LogP |
3.178
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
29
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| Complexity |
564
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CC1(CC2=C(O1)C(=CC(=C2N)Cl)C(=O)NC[C@@H]3CCN(C[C@H]3O)CCCOC)C
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| InChi Key |
FOUUNSGQVBGYQM-SUMWQHHRSA-N
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| InChi Code |
InChI=1S/C21H32ClN3O4/c1-21(2)10-15-18(23)16(22)9-14(19(15)29-21)20(27)24-11-13-5-7-25(12-17(13)26)6-4-8-28-3/h9,13,17,26H,4-8,10-12,23H2,1-3H3,(H,24,27)/t13-,17+/m0/s1
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| Chemical Name |
4-amino-5-chloro-N-[[(3S,4S)-3-hydroxy-1-(3-methoxypropyl)piperidin-4-yl]methyl]-2,2-dimethyl-3H-1-benzofuran-7-carboxamide
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| Synonyms |
SSP002358; SSP 002358; Revexepride; 219984-49-3; (-)-revexepride; revexeprida; SPD-557; SSP-002358
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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 : ≥ 100 mg/mL (~234.8 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3477 mL | 11.7385 mL | 23.4769 mL | |
| 5 mM | 0.4695 mL | 2.3477 mL | 4.6954 mL | |
| 10 mM | 0.2348 mL | 1.1738 mL | 2.3477 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.
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