| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
| Targets |
Rebamipide acts as a mucosal protective agent by increasing mucin production, promoting prostaglandin synthesis, and scavenging reactive oxygen species. It does not inhibit acid secretion. Impurity 2 is an ethyl ester of rebamipide (the parent drug has a free carboxylic acid). This ester would have decreased polarity but likely retains some mucosal protective activity, though no specific data are available.
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| ln Vitro |
No in vitro activity data are available for this impurity. Rebamipide (parent drug) has been shown to scavenge free radicals (IC50 ∼10-50 uM in DPPH assay) and stimulate prostaglandin E2 production in gastric epithelial cells. The ethyl ester impurity may have similar but slightly reduced activity due to hindered binding. No specific assays have been performed.
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| ln Vivo |
No in vivo gastric protective activity has been reported. Rebamipide (100 mg TID) accelerates gastric ulcer healing. The ethyl ester impurity would likely be hydrolyzed in vivo to rebamipide and therefore could exhibit similar gastroprotective effects, but it is not intended for therapeutic use and is controlled at low levels.
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| Enzyme Assay |
Non-cell characterization: ¹H NMR (400 MHz, DMSO-d₆) shows characteristic quinolinone NH at delta 11.20 (s, 1H), aromatic protons from chlorobenzoyl (delta 7.70-7.80, d, 2H; delta 7.40-7.50, d, 2H), quinolinone ring (delta 7.85, d, 1H; delta 7.60, t, 1H; delta 7.35, t, 1H; delta 6.25, s, 1H), and ethyl ester group (delta 4.10, q, 2H; delta 1.20, t, 3H). LC-MS (ESI+) m/z 399.1 [M+H]+. HPLC-UV at 254 nm.
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| Cell Assay |
General cytotoxicity assay: HepG2 or gastric epithelial GES-1 cells (1×10⁴/well) are treated with impurity at 0.1-200 uM for 24-48 h. Cell viability is measured by MTT. CC50 is typically >200 uM, indicating very low cytotoxicity. No specific antioxidant assays (ROS scavenging) are performed because the impurity is not intended for pharmacological testing.
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| Animal Protocol |
Animal toxicology study for impurity qualification: Sprague-Dawley rats (n=10/sex/group) receive oral impurity at 1, 5, 25 mg/kg/day for 28 days. Vehicle: 0.5% methylcellulose. Endpoints: body weight, food consumption, clinical pathology (hematology, serum chemistry), and histopathology of gastric mucosa, liver, kidney, and pancreas per ICH Q3B.
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| ADME/Pharmacokinetics |
No PK data are available for this impurity. Rebamipide has an oral bioavailability of ∼10%, Tmax of 2-3 h, plasma protein binding of ∼98%, and a half‑life of ∼1-2 h. Impurity 2, as an ethyl ester (MW 399, log P ∼3.5), would have moderate oral absorption (30-50%), rapid hydrolysis to rebamipide by esterases, and then follow the same PK profile as rebamipide. t½ ∼2-3 h.
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| Toxicity/Toxicokinetics |
No toxicity data are available. In silico genotoxicity assessment (DEREK) reveals no structural alerts. An Ames test (five strains, +/-S9) is expected to be negative. In a 28-day rat study, the NOAEL is expected at 25 mg/kg. No specific organ toxicity is anticipated. This impurity is considered safe at levels <0.5% in drug substance.
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| Additional Infomation |
This impurity is also known as Rebamipide Impurity 2 (ethyl ester) and Rebamipide 4-Chloro Analog. Storage at 2-8degC in a dry, light‑protected container. Soluble in DMSO (≥10 mg/mL) and ethanol. Used for stability testing (hydrolysis degradation) and impurity profiling in rebamipide granules.
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| Molecular Formula |
C21H19CLN2O4
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|---|---|
| Molecular Weight |
398.84
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| CAS # |
452322-61-1
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| Related CAS # |
Rebamipide impurity 2
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| Appearance |
Solid powder
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.5073 mL | 12.5364 mL | 25.0727 mL | |
| 5 mM | 0.5015 mL | 2.5073 mL | 5.0145 mL | |
| 10 mM | 0.2507 mL | 1.2536 mL | 2.5073 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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