Biological Activity
H+,K+-ATPase inhibitor (IC50 = 5.8 μM) that displays antisecretory and antiulcer activity. Inhibits gastric acid secretion (IC50 = 0.16 μM for histamine-induced acid formation) and reduces gastric lesion formation induced by a variety of ulcerative stimuli. Antibacteral against Helicobacter pylori in vitro. Also inhibits CYP2C19, CYP2C9 and CYP3A (Ki values are 3.1, 40.1 and 84.4 μM respectively) and blocks swelling-dependent chloride channels (ICIswell).
Technical Data
| M. Wt | 345.42 |
| Formula | C17H19N3O3S |
| Storage | Desiccate at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 73590-58-6 |
| PubChem ID | 4594 |
| InChI Key | SUBDBMMJDZJVOS-UHFFFAOYSA-N |
| Smiles | COC1=CC=C2N=C(NC2=C1)S(=O)CC1=C(C)C(OC)=C(C)C=N1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 1eq. HCl | 17.27 | 50 | |
| DMSO | 34.54 | 100 | |
| ethanol | 8.64 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 345.42. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.9 mL | 14.48 mL | 28.95 mL |
| 5 mM | 0.58 mL | 2.9 mL | 5.79 mL |
| 10 mM | 0.29 mL | 1.45 mL | 2.9 mL |
| 50 mM | 0.06 mL | 0.29 mL | 0.58 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Satoh et al (1989) Antisecretory and anitulcer activities of a novel proton pump inhibitor AG-1749 in dogs and rats. J.Pharmacol.Exp.Ther. 248 806 PMID: 2537418
Richardson et al (1998) Proton pump inhibitors. Drugs 56 307 PMID: 9777309
Schmarda et al (2000) The gastric H,K-ATPase blocker lansoprazole is an inhibitor of chloride channels. Br.J.Pharmacol. 129 598 PMID: 10711360
Keywords: Omeprazole, supplier, H+K+-ATPase, inhibitors, inhibits, Hydrogen, Potassium-ATPase, Ion, Transporters, Pumps, ATPases, cytochrome, p450, CYP2C19, CYP2C9, CYP3A, H+,K+-ATPase, Cytochrome, P450, H+,K+-ATPase, Tocris Bioscience
