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928774-43-0

928774-43-0 Structure

928774-43-0 Structure
IdentificationBack 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 PropertiesBack 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
Safety DataBack Directory
[WGK Germany ]

3
Hazard InformationBack 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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