For research use only. Not for therapeutic Use.
PF 03716556 is a potent, selective, competitive and reversible acid pump (H+,K+-ATPase) antagonist with pIC50s of 6.026, 6.038 and 6.009 for porcine, canine, and human recombinant gastric H+,K+-ATPase, respectively. PF 03716556 is inactive against other receptors, ion channels, and enzymes. PF 03716556 has the potential for gastroesophageal reflux disease research[1].
In porcine ion-tight membrane vesicles, PF 03716556 inhibits H+,K+-ATPase activity in a concentration-dependent manner, with a pIC50 value of 7.095 at pH 7.4[1].
PF 03716556 (1-10 mg/kg; intraduodenal administration; once; male Sprague-Dawley rats) treatment inhibits gastric acid secretion in a dose-dependent manner in rats[1].
| Catalog Number | I005523 |
| CAS Number | 928774-43-0 |
| Synonyms | 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 |
| Molecular Formula | C22H26N4O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C22H26N4O3/c1-14-5-4-6-19-20(14)17(7-10-29-19)24-18-11-16(22(28)25(3)8-9-27)13-26-12-15(2)23-21(18)26/h4-6,11-13,17,24,27H,7-10H2,1-3H3/t17-/m1/s1 |
| InChIKey | YBHKBMJREUZHOV-QGZVFWFLSA-N |
| SMILES | CC1=C2C(CCOC2=CC=C1)NC3=CC(=CN4C3=NC(=C4)C)C(=O)N(C)CCO |
| Reference | [1]. Hiroki Mori, et al. 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 gastroesophageal reflux disease. J Pharmacol Exp Ther. 2009 Feb;328(2):671-9. |
