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| PF03716556 Basic information |
| Product Name: | PF03716556 | | Synonyms: | 8-[[(4R)-3,4-Dihydro-5-Methyl-2H-1-benzopyran-4-yl]aMino]-N-(2-hydroxyethyl)-N,2-diMethyliMidazo[1,2-a]pyridine-6-carboxaMide;N-(2-Hydroxyethyl)-N,2-diMethyl-8-{[(4R)-5-Methyl-3,4-dihydro-2H-chroMen-4-yl]aMino}iMidazo[1,2-a]pyridine-6-carboxa;(R)-N-(2-hydroxyethyl)-N,2-dimethyl-8-(5-methyl-3,4-dihydro-2H-chromen-4-ylamino)H-imidazo[1,2-a]pyridine-6-carboxamide;8-[[(4R)-3,4-Dihydro-5-methyl-2H-1-benzopyran-4-yl]amino]-N-(2-hydroxyethyl)-N,2-dimethylimidazo[1,2-a]pyridine-6-carboxamide PF 03716556;[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];PF03716556;PF 3716556;PF-3716556;PF-03716556; PF03716556 | | CAS: | 928774-43-0 | | MF: | C22H26N4O3 | | MW: | 394.47 | | EINECS: | | Product Categories: | Amines;Aromatics;Heterocycles;Inhibitors;Intermediates & Fine Chemicals;Pfizer Compounds;Pharmaceuticals | | Mol File: | 928774-43-0.mol |
| PF03716556 Chemical Properties |
| Melting point | 143-145°C | | density | 1.30 | | storage temp. | Keep in dark place,Inert atmosphere,2-8°C | | solubility | DMSO: ≥10mg/mL | | form | powder | | pka | 14.18±0.10(Predicted) | | color | white to tan |
| PF03716556 Usage And Synthesis |
| Chemical Properties | Light Tan Solid | | Uses | A novel, potent, and selective acid pump antagonist for the treatment of gastroesophageal reflux disease. | | Biological Activity | the gastric h+,k+-atpase, which is responsible for gastric acid secretion, is a p2-type atpase located in the apical membrane of parietal cells. inhibition of the h+,k+-atpase is currently the most effective way to control gastric acid secretion and remains an attractive target for the medical treatment of acidrelated diseases. pf-03716556 is a novel, potent, and selective acid pump antagonist for the treatment of gastroesophageal reflux disease. | | in vitro | pf-03716556 demonstrated 3-fold greater inhibitory activity than revaprazan, the only acid pump antagonist that has been available on the market, in ion-tight assay. kinetics experiments revealed that pf-03716556 has a competitive and reversible mode of action [1]. | | in vivo | pf-03716556 did not display any species differences, exhibiting highly selective profile including the canine kidney h+,k+-atpase. in addition, more rapid onset of action than omeprazole and 3-fold greater potency than revaprazan were observed in ghosh-schild rats and heidenhain pouch dogs [2]. | | IC 50 | in porcine ion-tight membrane vesicles, pf-03716556 inhibited h+,k+-atpase activity in a concentration-dependent manner, with a pic50 value of 7.095 ± 0.077 at ph 7.4. | | references | [1] mori h, tonai-kachi h, ochi y, taniguchi y, ohshiro h, takahashi n, aihara t, hirao a, kato t, sakakibara m, kurebayashi y. 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;328(2):671-9. |
| PF03716556 Preparation Products And Raw materials |
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