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10mg |
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Other Sizes |
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Rabeprazole (LY-307640) is a novel, potent and 2nd-generationproton pump inhibitor (PPI) that is used as an antiulcer drug. Itirreversibly inactivates gastric H+/K+-ATPase and inducesapoptosis. Rabeprazole acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with anIC50of 0.3 μM. Rabeprazole can be used for the research of gastric ulcerations and gastroesophageal reflux.It is a partially reversible gastric proton pump inhibitor and also an inhibitor of ATP4.
ln Vitro |
Following a 16-hour exposure to 0.2 mM of rabeprazole, human gastric cancer cells exhibit reduced vitality [2]. In MKN-28 cells, rabeprazole totally suppressed ERK1/2 phosphorylation. For two hours, the gastric cancer cell line MKN-28 was grown in an acidic media (pH 5.4). In MKN-28 cells, rabeprazole pretreatment (0.2 mM, 2 hours) significantly reduced ERK1/2 phosphorylation [2].
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ln Vivo |
In female mice, courses of rabeprazole (10 mg/kg; oral; every 48 hours for 18 weeks) led to significant reductions in serum calcium levels, secondary parathyroid disease, and bone mineral density (BMD). hyperthyroidism [3].
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Cell Assay |
Cell Viability Assay[2]
Cell Types: Three gastric cancer cell lines KATO III, MKN-28 and MKN-45 Tested Concentrations: 0.2 mM Incubation Duration: 16 hrs (hours) Experimental Results: Treatment resulted in diminished viability of all cancer cell lines tested, with KATO III and Compared with MKN-45 cells, the cell viability of MKN-28 cells was Dramatically diminished. Cell viability assay[2] Cell Types: Three gastric cancer cell lines (KATO III, MKN-28 and MKN-45)[2] Tested Concentrations: 0.2 mM Incubation Duration: 2 hrs (hours) pretreatment Experimental Results: Result in strong inhibition of ERK 1/2 Phosphorylated in MKN-28 cells, but no similar effect was observed in KATO III and MKN-45 cells. |
Animal Protocol |
Animal/Disease Models: Female Swiss albino mice (body weight 18-26 g) [3]
Doses: 10 mg/kg Route of Administration: Oral; every 48 hrs (hrs (hours)) for 18 weeks Experimental Results: Serum calcium levels compared with vehicle-treated group Dramatically lower (5.5±2.07 vs. 9.68±2.77). |
References |
[1]. Tara A Shea, et al. Identification of Proton-Pump Inhibitor Drugs That Inhibit Trichomonas Vaginalis Uridine Nucleoside Ribohydrolase. Bioorg Med Chem Lett. 2014 Feb 15;24(4):1080-4.
[2]. Mengli Gu, et al. Rabeprazole Exhibits Antiproliferative Effects on Human Gastric Cancer Cell Lines. Oncol Lett. 2014 Oct;8(4):1739-1744. [3]. Aly A M Shaalan, et al. Supplement With Calcium or Alendronate Suppresses Osteopenia Due to Long Term Rabeprazole Treatment in Female Mice: Influence on Bone TRAP and Osteopontin Levels. Front Pharmacol. 2020 May 13;11:583. |
Molecular Formula |
C18H21N3O3S
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Molecular Weight |
359.4426
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CAS # |
117976-89-3
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Related CAS # |
Rabeprazole sodium;117976-90-6;Rabeprazole-d4;934295-48-4;Rabeprazole Sulfide;117977-21-6
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
S(C1=NC2=C([H])C([H])=C([H])C([H])=C2N1[H])(C([H])([H])C1C(C([H])([H])[H])=C(C([H])=C([H])N=1)OC([H])([H])C([H])([H])C([H])([H])OC([H])([H])[H])=O
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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 | 2.7821 mL | 13.9105 mL | 27.8211 mL | |
5 mM | 0.5564 mL | 2.7821 mL | 5.5642 mL | |
10 mM | 0.2782 mL | 1.3911 mL | 2.7821 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.