| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| Other Sizes |
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| ln Vitro |
H 16868, also known as omeprazole, is a proton pump inhibitor that is used to treat Zollinger-Ellison syndrome, dyspepsia, peptic ulcer disease, and gastroesophageal reflux disease. Mean hourly hydrogen ion activity dropped from 38.50 to 1.95 mmol(mEq)/1 (p less than 0.001), and median 24-hour gastric pH increased from 1.4 to 5.3 in all patients treated with omeprazole (H 16868), practically eliminating gastric acidity. More significant than the effects of ranitidine 300 mg daily or cimetidine 1 g daily, which have been documented earlier, is this inhibitory effect on 24-hour gastric acidity [1]. A group of healthy male volunteers were tested to examine the pharmacokinetics of single and repeated oral dosages of 30 and 60 mg of omeprazole. The unpredictable absorption of omeprazole (H 16868) from its enteric-coated formulation occurs. The plasma concentration-time curve's (AUC) area under the curve (AUC) considerably increased following repeated dosage. Once dosed repeatedly, omeprazole (H 16868) increases its relative availability. Omeprazole, an acid-labile substance, may be to blame for this, as it inhibits the release of gastric acid [2]. An effective inhibitor of neutral sphingomyelinase (N-SMase) and exosome that can penetrate the brain is omeprazole sodium [3].
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| References |
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| Additional Infomation |
Omeprazole sodium is a member of benzimidazoles and a sulfoxide.
Omeprazole Sodium is the sodium salt form of a benzimidazole with selective and irreversible proton pump inhibitor activity. In the acidic compartment of parietal cells, omeprazole is protonated and converted into the active achiral sulfenamide; the active sulfenamide forms one or more covalent disulfide bonds with the proton pump hydrogen-potassium adenosine triphosphatase (H+/K+ ATPase), thereby inhibiting its activity and the parietal cell secretion of H+ ions into the gastric lumen, the final step in gastric acid production. H+/K+ ATPase is an integral membrane protein of the gastric parietal cell. Esomeprazole Sodium is the sodium salt of the S-isomer of omeprazole, with gastric proton pump inhibitor activity. In the acidic compartment of parietal cells, esomeprazole is protonated and converted into the active achiral sulfenamide; the active sulfenamide forms one or more covalent disulfide bonds with the proton pump hydrogen-potassium adenosine triphosphatase (H+/K+ ATPase), thereby inhibiting its activity and the parietal cell secretion of H+ ions into the gastric lumen, the final step in gastric acid production. H+/K+ ATPase is an integral membrane protein of the gastric parietal cell. A 4-methoxy-3,5-dimethylpyridyl, 5-methoxybenzimidazole derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits an H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS. See also: Omeprazole (has active moiety). |
| Molecular Formula |
C17H18N3NAO3S
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|---|---|
| Molecular Weight |
367.3979
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| Exact Mass |
385.107
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| CAS # |
95510-70-6
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| Related CAS # |
Omeprazole;73590-58-6;Omeprazole-d3;922731-01-9;Omeprazole magnesium;95382-33-5
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| PubChem CID |
10959536
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| Appearance |
White to off-white solid powder
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| Density |
1.37g/cm3
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| Boiling Point |
600ºC at 760mmHg
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| Melting Point |
220°C
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| Flash Point |
316.7ºC
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| LogP |
3.486
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
25
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| Complexity |
459
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
RYXPMWYHEBGTRV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H18N3O3S.Na/c1-10-8-18-15(11(2)16(10)23-4)9-24(21)17-19-13-6-5-12(22-3)7-14(13)20-17;/h5-8H,9H2,1-4H3;/q-1;+1
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| Chemical Name |
sodium;5-methoxy-2-[(4-methoxy-3,5-dimethylpyridin-2-yl)methylsulfinyl]benzimidazol-1-ide
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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) |
DMSO : ~125 mg/mL (~340.23 mM)
H2O : ~5.56 mg/mL (~15.13 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.66 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 20.8 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: ≥ 2.08 mg/mL (5.66 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: 2.08 mg/mL (5.66 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7218 mL | 13.6091 mL | 27.2183 mL | |
| 5 mM | 0.5444 mL | 2.7218 mL | 5.4437 mL | |
| 10 mM | 0.2722 mL | 1.3609 mL | 2.7218 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00674115 | COMPLETEDWITH RESULTS | Drug: Omeprazole/sodium bicarbonate Drug: omeprazole magnesium Drug: sodium bicarbonate |
Gastric Acid Human Experimentation |
Bayer | 2008-04 | Phase 3 |
| NCT00428701 | COMPLETED | Drug: Esomeprazole Sodium | Gastric Ulcer | AstraZeneca | 2006-10 | Phase 4 |
| NCT00765206 | COMPLETEDWITH RESULTS | Drug: Omeprazole/sodium bicarbonate Drug: omeprazole magnesium (20 mg equivalent) |
Gastric Acid Human Experimentation |
Bayer | 2008-05 | Phase 3 |
| NCT00808769 | COMPLETEDWITH RESULTS | Drug: Zegerid® Drug: Prilosec OTC® |
Normal Healthy Subject Population | Procter and Gamble | 2008-11 | Phase 4 |
| NCT01710995 | COMPLETED | Drug: Zegerid Drug: Losec |
Acid Reflux Gastro Oesophageal Reflux Disease |
Norgine | 2010-10 | Phase 1 |
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