Biological Activity
H+,K+-ATPase inhibitor (IC50 = 6.3 μM) that displays antisecretory and antiulcer activity. Inhibits gastric acid secretion (IC50 = 0.09 μM for histamine-induced acid formation) and reduces gastric lesion formation induced by a variety of ulcerative stimuli. Antibacterial against Helicobacter pylori in vitro. Also blocks swelling-dependent chloride channel (ICIswell) in NIH3T3 fibroblasts. More potent than omeprazole (Cat. No. 2583).
Technical Data
| M. Wt | 369.36 |
| Formula | C16H14F3N3O2S |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 103577-45-3 |
| PubChem ID | 3883 |
| InChI Key | MJIHNNLFOKEZEW-UHFFFAOYSA-N |
| Smiles | CC1=C(OCC(F)(F)F)C=CN=C1CS(=O)C1=NC2=CC=CC=C2N1 |
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 | 18.47 | 50 | |
| DMSO | 36.94 | 100 | |
| ethanol | 18.47 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 369.36. 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 | 2.71 mL | 13.54 mL | 27.07 mL |
| 5 mM | 0.54 mL | 2.71 mL | 5.41 mL |
| 10 mM | 0.27 mL | 1.35 mL | 2.71 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.54 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Satoh et al (1989) Antisecretory and antiulcer activities of a novel proton pump inhibitor AG-1749 in dogs and rats. J.Pharmacol.Exp.Ther. 248 806 PMID: 2537418
Schmarda et al (2000) The gastric H,K-ATPase blocker lansoprazole is an inhibitor of chloride channels. Br.J.Pharmacol. 129 598 PMID: 10711360
Matheson and Jarvis (2001) Lansoprazole. Drugs 61 1801 PMID: 11693467
Keywords: Lansoprazole, supplier, H+K+-ATPase, inhibitors, inhibits, Hydrogen, Potassium-ATPase, Ion, Transporters, Pumps, ATPases, AG1749, AG-1749, H+,K+-ATPase, H+,K+-ATPase, Tocris Bioscience
