Identification | Back Directory | [Name]
PF03716556 | [CAS]
928774-43-0 | [Synonyms]
CS-1022 PF03716556 PF 3716556 PF03716556 USP/EP/BP PF-03716556; PF03716556 PF3716556/PF-3716556/PF-03716556 PF-3716556;PF-03716556; PF03716556 (R)-N-(2-Hydroxyethyl)-N,2-dimethyl-8-((5-methylchroman-4-yl)amino)imidazo[1,2-a]pyridine-6-ca 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 [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] 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 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-dimethyl- 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 | [Molecular Formula]
C22H26N4O3 | [MDL Number]
MFCD19690947 | [MOL File]
928774-43-0.mol | [Molecular Weight]
394.47 |
Chemical Properties | Back Directory | [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 |
Hazard Information | Back Directory | [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. | [storage]
Store at -20°C | [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. |
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NCE Biomedical Co.,Ltd.
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