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| Targets |
Rabeprazole-d4 sodium targets the H+/K+-ATPase enzyme (proton pump) in gastric parietal cells. The parent compound, Rabeprazole, is a prodrug that is converted to its active form in the acidic environment of the parietal cell canaliculus. It then binds covalently to cysteine residues on the H+/K+-ATPase, irreversibly inhibiting gastric acid secretion. The deuterated version has the same mechanism and is used as an internal standard for quantification.
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| ln Vitro |
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as tracers for quantification throughout the drug development process. Due to its potential to alter the pharmacokinetic and metabolic characteristics of medications, deuteration has drawn attention[1].
Rabeprazole-d4 sodium is a deuterated compound used as an internal standard for LC-MS/MS quantification. The non-deuterated parent, Rabeprazole, is a potent proton pump inhibitor. In vitro, it blocks the final step of gastric acid secretion by inhibiting the H+/K+-ATPase enzyme. It has an IC50 value of approximately 0.7 microM in isolated gastric glands. Rabeprazole is also a weak inhibitor of CYP2C19 and CYP3A4. |
| ln Vivo |
In vivo, Rabeprazole is used to treat acid-related disorders such as GERD and peptic ulcers. It is effective at suppressing basal and stimulated gastric acid secretion. The deuterated version is used as an internal standard for PK studies. Rabeprazole has an oral bioavailability of approximately 52% in humans and a plasma half-life of about 1-2 hours. The compound is extensively metabolized by CYP2C19 and CYP3A4.
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| Enzyme Assay |
Rabeprazole-d4 sodium is used as an internal standard for LC-MS/MS. A fixed concentration (e.g., 50-100 ng/mL) of the d4 internal standard is added to biological samples (e.g., plasma, urine). Samples are extracted by protein precipitation or liquid-liquid extraction. LC-MS/MS analysis is performed on a C18 column with a mobile phase of water/acetonitrile (0.1% formic acid). Detection is in positive ion mode (ESI+). Rabeprazole is monitored using MRM transitions (e.g., m/z 360 → 242). The d4 internal standard has a mass shift of +4 Da (m/z 364 → 246). The peak area ratio is used for quantification.
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| Cell Assay |
Rabeprazole-d4 sodium is not used in typical cell-based assays. The non-deuterated parent, Rabeprazole, can be used to study its effects on acid secretion in gastric parietal cell cultures. Human gastric cancer cells (e.g., HGT-1) are seeded in 24-well plates and treated with Rabeprazole (1-100 microM) for 30-60 min. The activity of H+/K+-ATPase is measured by determining the release of inorganic phosphate from ATP. The IC50 is calculated.
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| Animal Protocol |
Rabeprazole-d4 sodium is used as an internal standard for PK studies of Rabeprazole. A standard animal protocol: male Sprague-Dawley rats (200-250 g) are administered a single oral dose of Rabeprazole sodium (1-10 mg/kg) in 0.5% methylcellulose. Blood samples are collected at pre-dose and at 0.25, 0.5, 1, 2, 4, 6, 8, 12, 24 h post-dose. Plasma is separated. A fixed concentration of Rabeprazole-d4 sodium is added to each sample. Samples are extracted and analyzed by LC-MS/MS. PK parameters are calculated using non-compartmental analysis.
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| ADME/Pharmacokinetics |
Rabeprazole-d4 sodium has a molecular weight of 385.45 and the molecular formula C18H16D4N3NaO3S. The product should be stored at 4degC, sealed, and away from moisture. In solvent, it is stable for 6 months at -80degC or 1 month at -20degC. The compound has a purity of ≥98%. Specific PK parameters are available for the parent compound.
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| Toxicity/Toxicokinetics |
Rabeprazole is generally well-tolerated. Common adverse effects include headache, diarrhea, and nausea. Long-term use may increase the risk of vitamin B12 deficiency and bone fractures. The deuterated version is used in trace amounts as an analytical standard and does not pose additional safety risks beyond standard chemical handling. Standard safety precautions for handling PPIs should be followed.
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| References |
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| Additional Infomation |
Rabeprazole-d4 sodium is a research-grade stable isotope-labeled compound and is not approved for clinical use. It is used as an internal standard for the quantification of Rabeprazole, a proton pump inhibitor. This product is for research use only and not for human therapeutic applications. Store as a powder at 4degC. The sodium salt form enhances solubility.
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| Molecular Formula |
C18H16D4N3NAO3S
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| Molecular Weight |
385.45
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| Related CAS # |
Rabeprazole sodium;117976-90-6;Rabeprazole-d3 sodium;1216494-11-9
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| Appearance |
Light yellow to yellow 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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 | 2.5944 mL | 12.9719 mL | 25.9437 mL | |
| 5 mM | 0.5189 mL | 2.5944 mL | 5.1887 mL | |
| 10 mM | 0.2594 mL | 1.2972 mL | 2.5944 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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