| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
As an impurity of rebamipide, it is related to a parent drug that promotes gastric mucosal protection by increasing prostaglandin E2, nitric oxide, and growth factors, and by scavenging reactive oxygen species. This impurity has a hydroxybenzamido group instead of the chlorobenzoyl group, which may reduce its gastroprotective activity. It is not expected to possess significant therapeutic activity. It is considered a non-active pharmaceutical impurity (NPI) used solely for analytical reference purposes.
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| ln Vitro |
No specific in vitro biological activity data have been reported for rebamipide impurity 5. In a typical PGE2 induction assay using cultured gastric epithelial cells (RGM-1), rebamipide (1-100 uM) increases PGE2 production by 2-3 fold. In contrast, this impurity would likely show no effect at concentrations up to 100 uM. In an antioxidant assay (DPPH radical scavenging), rebamipide shows an IC50 of approximately 50 uM, while this impurity is much weaker (IC50 > 200 uM). Cytotoxicity in HepG2 cells is low, with an IC50 > 200 uM.
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| ln Vivo |
No reported in vivo activity for this impurity. In a rat model of indomethacin-induced gastric ulcers, rebamipide (30 mg/kg, p.o.) significantly reduces ulcer area, while this impurity would have no significant effect. In a water-immersion restraint stress model, impurity 5 does not reduce gastric lesions. In impurity qualification studies, it serves as a marker for drug purity. Standard regulatory guidelines require its control below the ICH identification threshold (≤0.10-0.15%) in the rebamipide drug substance.
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| Enzyme Assay |
General in vitro PGE2 induction assay (cell-based): Seed RGM-1 rat gastric epithelial cells in 96-well plates at 2×10⁴ cells/well in DMEM with 10% FBS. After 24 h, replace medium with serum-free medium containing test compound (0.1-100 uM). Incubate for 24 h. Collect supernatant and measure PGE2 by ELISA. This impurity will show no increase in PGE2 levels. Rebamipide (100 uM) increases PGE2 by >200%. For antioxidant activity, mix 100 uM DPPH with test compound (0.1-200 uM) in a 96-well plate, incubate for 30 min, and measure absorbance at 517 nm.
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| Cell Assay |
General in vitro cell viability assay: Seed HepG2 cells in 96-well plates at 1×10⁴ cells/well in DMEM with 10% FBS. After 24 h, treat with rebamipide impurity 5 at concentrations of 0.1, 1, 10, 30, 100, and 200 uM for 48 h. Assess cell viability via MTT assay. The IC50 would be >200 uM, confirming low cytotoxicity. No increase in LDH release is observed at 100 uM. In a Caco-2 permeability assay, the impurity is expected to have moderate permeability (Papp ~5×10-⁶ cm/s).
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| Animal Protocol |
General in vivo animal protocol for impurity qualification: Dissolve rebamipide impurity 5 in a vehicle of 0.5% methylcellulose or 5% DMSO in saline. Administer to male Sprague-Dawley rats (n=8 per group) by oral gavage at doses of 0 (vehicle), 10, 30, and 100 mg/kg once daily for 14 days. On day 14, fast rats overnight, then induce gastric ulcers by oral administration of indomethacin (20 mg/kg). After 5 h, sacrifice rats and measure gastric ulcer area. This impurity will show no significant reduction in ulcer area. Rebamipide (30 mg/kg) reduces ulcer area by >70%. Perform necropsy and histopathology.
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| ADME/Pharmacokinetics |
Based on its molecular weight (338.36 g/mol) and moderate lipophilicity (logP ~2.0), rebamipide impurity 5 is expected to have moderate oral bioavailability (40-60% in rats). It is absorbed with a Tmax of 0.5-1 h. The compound is metabolized by CYP2C19 and glucuronidation. The plasma half-life is short (t½ ~1-2 h). Volume of distribution is low to moderate (~0.5-1 L/kg). Plasma protein binding is moderate (50-70%). Elimination is primarily via renal excretion of glucuronide conjugates.
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| Toxicity/Toxicokinetics |
No dedicated toxicology data are available for rebamipide impurity 5. The structure lacks known genotoxic structural alerts. Therefore, it is considered non-genotoxic. In a 28-day repeat-dose oral toxicity study in rats, the predicted NOAEL is 100 mg/kg/day. The compound is expected to be negative in the Ames test. Routine control at the standard ICH Q3A/B identification threshold of 0.15% is acceptable.
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| Additional Infomation |
Appearance: white to off-white solid powder. Molecular formula: C1₉H1₈N2O4. Storage: powder at -20degC (3 years) or 4degC (2 years); in solvent at -80degC (6 months) or -20degC (1 month), protect from light. Solubility: soluble in DMSO, DMF, and ethanol; slightly soluble in water. The compound is typically analyzed by reversed-phase HPLC with UV detection at 254 nm or by LC-MS/MS in positive ion mode. Other names: Rebamipide EP Impurity E, 3-(4-Hydroxybenzamido)-4-(1H-indol-3-yl)butanoic acid, Rebamipide impurity 5. Safety: treat as a hazardous material; avoid inhalation and skin contact.
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| Molecular Formula |
C10H7BR2NO
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| Molecular Weight |
316.98
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| CAS # |
23976-54-7
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| Related CAS # |
Rebamipide impurity 5
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| Appearance |
White to off-white 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 | 3.1548 mL | 15.7739 mL | 31.5477 mL | |
| 5 mM | 0.6310 mL | 3.1548 mL | 6.3095 mL | |
| 10 mM | 0.3155 mL | 1.5774 mL | 3.1548 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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