| 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 |
[1]. Li XQ, et al. Comparison of inhibitory effects of the proton pump-inhibiting drugs omeprazole, esomeprazole, lansoprazole, pantoprazole, and rabeprazole on human cytochrome P450 activities. Drug Metab Dispos. 2004 Aug;32(8):821-7.
[2]. Jonkers D, et al. Omeprazole inhibits growth of gram-positive and gram-negative bacteria including Helicobacter pylori in vitro. J Antimicrob Chemother. 1996 Jan;37(1):145-50. [3]. Huarui Zhang, et al. Advances in the discovery of exosome inhibitors in cancer. J Enzyme Inhib Med Chem. 2020 Dec;35(1):1322-1330. |
| Molecular Formula |
C17H18N3NAO3S
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|---|---|
| Molecular Weight |
367.3979
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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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| SMILES |
S(C1=NC2C([H])=C([H])C(=C([H])C=2[N-]1)OC([H])([H])[H])(C([H])([H])C1C(C([H])([H])[H])=C(C(C([H])([H])[H])=C([H])N=1)OC([H])([H])[H])=O.[Na+]
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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 : ~125 mg/mL (~340.23 mM)
H2O : ~5.56 mg/mL (~15.13 mM) |
|---|---|
| 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.
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