Biological Activity
H+,K+-ATPase inhibitor (pIC50 = 6 in human recombinant ion-leaky assays); more potent in acidic conditions. Highly selective for H+,K+-ATPase in vitro; displays no activity at Na+,K+-ATPase. Also displays selectivity for H+,K+-ATPase over a range of 50 receptors and ion channels (IC50 > 10 μM). Inhibits gastric acid secretion in rat and dog models.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Technical Data
| M. Wt | 394.47 |
| Formula | C22H26N4O3 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 928774-43-0 |
| PubChem ID | 25134521 |
| InChI Key | YBHKBMJREUZHOV-QGZVFWFLSA-N |
| Smiles | OCCN(C)C(C2=CN1C(C(N[C@H]4C3=C(C)C=CC=C3OCC4)=C2)=NC(C)=C1)=O |
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 | |||
| DMSO | 39.45 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 394.47. 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 | 2.54 mL | 12.68 mL | 25.35 mL |
| 5 mM | 0.51 mL | 2.54 mL | 5.07 mL |
| 10 mM | 0.25 mL | 1.27 mL | 2.54 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.51 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Mori et al (2009) N-(2-hydroxyethyl)-N,2-dimethyl-8-{[(4R)-5-methyl-3,4-dihydro-2H-chromen-4-yl]amino}imidazo[1,2-a]pyridine-6-carboxamide (PF-03716556), a novel, potent, and selective acid pump antagonist for the treatment of gastroesop J.Pharmacol.Exp.Ther. 328 671 PMID: 18981288
Keywords: PF 3716556, supplier, selective, inhibitors, inhibits, H+K+-ATPase, hydrogen, potassium-ATPase, ion, transporters, pumps, ATPases, PF3716556, pfizer, H+,K+-ATPase, H+,K+-ATPase, Tocris Bioscience
