| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Targets |
Rebamipide mofetil is an orally active prodrug that releases Rebamipide, which is the active pharmacological agent. The primary mechanism of action is mediated through Rebamipide's ability to induce COX-2 expression, which leads to increased production of prostaglandin E2 (PGE2). This enhances gastric mucosal defense mechanisms in a COX-2-dependent manner. The compound also stimulates prostaglandin production, mucus secretion, and epithelial regeneration, all of which contribute to mucosal protection. The prodrug design improves oral absorption and bioavailability compared to the parent compound.
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| ln Vitro |
In vitro studies demonstrate that Rebamipide, the active metabolite released from the prodrug, induces COX-2 expression in gastric epithelial cells. This leads to increased production of prostaglandin E2 (PGE2), a key mediator of gastric mucosal defense. The compound also stimulates mucus secretion and promotes epithelial regeneration in cell-based assays. These in vitro activities contribute to its mucoprotective effects. The prodrug itself, Rebamipide mofetil, is designed to be metabolically converted to the active parent drug in vivo, and its in vitro activity is assessed indirectly through the activity of its metabolite.
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| ln Vivo |
In vivo, Rebamipide mofetil is orally active and functions as a prodrug of Rebamipide (OPC12759). Following oral administration, it is metabolized to release the active parent drug, which then exerts its mucoprotective effects. Rebamipide enhances gastric mucosal defense by stimulating prostaglandin production, increasing mucus secretion, and promoting epithelial regeneration. The compound has been shown to induce COX-2 expression, increase PGE2 levels, and enhance gastric mucosal defense in a COX-2-dependent manner. It is being explored for gastrointestinal and ophthalmic disorders, offering improved absorption and sustained mucosal protection compared to conventional Rebamipide formulations.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for Rebamipide mofetil typically focus on its active metabolite, Rebamipide. The parent compound induces COX-2 expression in gastric epithelial cells, which is a key mechanism of action. Non-cellular assays may involve measuring the production of prostaglandin E2 (PGE2) in response to Rebamipide treatment, as well as assessing its effects on COX-2 enzyme activity. These assays help characterize the molecular mechanism by which Rebamipide enhances gastric mucosal defense. The prodrug itself is not directly active in these assays but is designed to release the active metabolite.
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| Cell Assay |
In vitro cellular assays for Rebamipide mofetil involve treating gastric epithelial cells with the compound and measuring downstream effects such as COX-2 expression, PGE2 production, and mucus secretion. The compound induces COX-2 expression and increases PGE2 levels in a dose-dependent manner. Cell viability and proliferation assays may also be performed to assess the cytoprotective effects of the compound. These cell-based studies are essential for understanding the mucoprotective mechanism of the active metabolite. The prodrug is typically evaluated in cell-based systems that can metabolize it to the active parent compound.
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| Animal Protocol |
In vivo animal models for Rebamipide mofetil typically involve inducing gastric mucosal injury in rodents, followed by oral administration of the prodrug. Efficacy is assessed by measuring parameters such as gastric lesion area, mucosal blood flow, prostaglandin levels, and mucus production. The compound is administered orally, and its effects are compared to those of the parent drug Rebamipide. These studies demonstrate that the prodrug offers improved oral absorption and sustained mucosal protection compared to conventional formulations. Doses and administration routes are optimized based on the specific animal model and experimental endpoints.
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| ADME/Pharmacokinetics |
Rebamipide mofetil is an orally active prodrug designed to improve the pharmacokinetic properties of Rebamipide. Following oral administration, it is metabolized to release the active parent drug, Rebamipide (OPC12759). The prodrug approach offers improved absorption and bioavailability compared to the parent compound. The active metabolite has a favorable pharmacokinetic profile characterized by good oral absorption and distribution to the gastrointestinal mucosa. The compound is metabolized to its active form and is being explored for gastrointestinal and ophthalmic disorders. The prodrug design enhances systemic exposure and therapeutic efficacy.
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| Toxicity/Toxicokinetics |
Rebamipide mofetil is a prodrug of Rebamipide, a mucoprotective agent with a well-established safety profile. The parent drug, Rebamipide, has been used clinically for the treatment of gastric ulcers and gastritis with a favorable safety record. The prodrug form is expected to have a similar safety profile, with potential adverse effects related to the gastrointestinal system. As with any drug, the safety of Rebamipide mofetil should be evaluated in preclinical toxicology studies. The compound is being explored for gastrointestinal and ophthalmic disorders, offering improved absorption compared to conventional Rebamipide formulations.
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| References | |
| Additional Infomation |
Rebamipide mofetil (CAS# 1527495-76-6) is an orally active prodrug of Rebamipide (OPC12759), a well-established mucoprotective agent. Rebamipide induces COX-2 expression, increases PGE2 levels, and enhances gastric mucosal defense in a COX-2-dependent manner. The prodrug approach improves oral absorption and bioavailability, offering sustained mucosal protection compared to conventional Rebamipide formulations. It is being explored for gastrointestinal and ophthalmic disorders. The compound is for research use only and is not approved for human therapeutic use. It represents a promising strategy to enhance the delivery and efficacy of Rebamipide.
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| Molecular Formula |
C25H26CLN3O5
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| Molecular Weight |
483.9440
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| Exact Mass |
483.156
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| CAS # |
1527495-76-6
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| PubChem CID |
86296442
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
743.9±60.0 °C at 760 mmHg
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| Flash Point |
403.7±32.9 °C
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| Vapour Pressure |
0.0±2.6 mmHg at 25°C
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| Index of Refraction |
1.630
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| LogP |
3.06
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
34
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| Complexity |
762
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
BVZOVIJSRAGQLP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H26ClN3O5/c26-19-7-5-17(6-8-19)24(31)28-22(25(32)34-14-11-29-9-12-33-13-10-29)15-18-16-23(30)27-21-4-2-1-3-20(18)21/h1-8,16,22H,9-15H2,(H,27,30)(H,28,31)
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| Chemical Name |
2-morpholin-4-ylethyl 2-[(4-chlorobenzoyl)amino]-3-(2-oxo-1H-quinolin-4-yl)propanoate
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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 (~206.64 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.17 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 (5.17 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.17 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0664 mL | 10.3319 mL | 20.6637 mL | |
| 5 mM | 0.4133 mL | 2.0664 mL | 4.1327 mL | |
| 10 mM | 0.2066 mL | 1.0332 mL | 2.0664 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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