| Size | Price | Stock | Qty |
|---|---|---|---|
| 5g |
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| Other Sizes |
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| ln Vitro |
The drug rebamipide (1.4, 2.7, 5.4 mM; 24 h) suppresses the growth of cells [1]. In AGS cells, rebamipide (5.4 mM; 30 min) activates Smad signal blue [1]. Rebamipide in AGS (5.4 mM; 3 h)
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|---|---|
| ln Vivo |
Rebamipide (5, 15, 50 mg/kg; once daily for 14 days in a row) protects the right side of the stomach mucosa from acid injury and increases the expression of COX-2 and PGE2 in the gastric mucosa [2].
|
| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: AGS cells Tested Concentrations: 1.4, 2.7, 5.4 mM Incubation Duration: 24 h Experimental Results: Cell proliferation was Dramatically diminished in a concentration-dependent manner. . Western Blot Analysis[1] Cell Types: AGS Cell Tested Concentrations: 5.4 mM Incubation Duration: 30 minutes or 3 hrs (hours) Experimental Results: The phosphorylation of Smad2/3 Dramatically increased 1.2-fold at 30 minutes, and the Smad2/3-Smad4 complex was formed 1.4 times. At 3 hrs (hours), the expression of p21 protein was up-regulated 2.5-fold. |
| Animal Protocol |
Animal/Disease Models: Specific pathogen-free male SD (SD (Sprague-Dawley)) rats (200-230 g; 7 weeks old) [2].
Doses: 5, 15, 50 mg/kg Route of Administration: Oral; one time/day for 14 days. Experimental Results: COX-2 immunoreactivity and PGE2 levels increased in a dose-dependent manner. (PGE2 is associated with protecting the gastric mucosa from various injuries and accelerating gastric wound healing). Inhibits gastric mucosal bleeding and erosion caused by intragastric (po) (po)administration of HCl. |
| References | |
| Additional Infomation |
2-[[(4-chlorophenyl)-oxomethyl]amino]-3-(2-oxo-1H-quinolin-4-yl)propanoic acid is a secondary carboxamide.
Rebamipide has been investigated for the treatment of Stomach Ulcer, Keratoconjunctivitis Sicca, and Gastric Adenoma and Early Gastric Cancer. Rebamipide is a quinolinone derivative with anti-ulcer and anti-inflammatory activities. Rebamipide induces cyclooxygenase 2 (COX2) synthesis which results in an increase in endogenous prostaglandin synthesis in the gastric mucosa. This agent also inhibits H. pylori-induced production of tumor necrosis factor (TNF) alpha and subsequent inflammation of the gastric mucosa. In addition, rebamipide scavenges oxygen-derived free radicals that potentially cause mucosal injury, and stimulates prostaglandin EP4 receptor gene expression followed by mucous secretion, thereby enhancing the gastric mucosal defense. |
| Molecular Formula |
C19H15CLN2O4
|
|---|---|
| Molecular Weight |
370.78
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| Exact Mass |
370.072
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| CAS # |
90098-04-7
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| Related CAS # |
Rebamipide-d4;1219409-06-9
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| PubChem CID |
5042
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
695.0±55.0 °C at 760 mmHg
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| Melting Point |
288-290ºC dec.
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| Flash Point |
374.1±31.5 °C
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| Vapour Pressure |
0.0±2.3 mmHg at 25°C
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| Index of Refraction |
1.634
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| LogP |
2.9
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
26
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| Complexity |
598
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ALLWOAVDORUJLA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H15ClN2O4/c20-13-7-5-11(6-8-13)18(24)22-16(19(25)26)9-12-10-17(23)21-15-4-2-1-3-14(12)15/h1-8,10,16H,9H2,(H,21,23)(H,22,24)(H,25,26)
|
| Chemical Name |
2-[(4-chlorobenzoyl)amino]-3-(2-oxo-1H-quinolin-4-yl)propanoic acid
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| Synonyms |
Mucosta; Proamipide; Rebamipide
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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 : ~33.33 mg/mL (~89.89 mM)
H2O : ~0.1 mg/mL (~0.27 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.74 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 (6.74 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 | 2.6970 mL | 13.4851 mL | 26.9702 mL | |
| 5 mM | 0.5394 mL | 2.6970 mL | 5.3940 mL | |
| 10 mM | 0.2697 mL | 1.3485 mL | 2.6970 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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