928774-43-0

Basic information

• Product Name: PF03716556
• Synonyms: PF03716556;PF 3716556;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;PF3716556/PF-3716556/PF-03716556;(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]
• CAS NO: 928774-43-0
• Molecular Formula: C22H26N4O3
• Molecular Weight: 394.46684
• EINECS: -0
• Product Categories: Amines;Aromatics;Heterocycles;Inhibitors;Intermediates & Fine Chemicals;Pfizer Compounds;Pharmaceuticals
• Mol File: 928774-43-0.mol
• Article Data: 0

Chemical Properties

• Melting Point: 143-145°C
• Appearance: white to tan/
• Density: 1.30
• Storage Temp.: Refrigerator
• Solubility: DMSO: ≥10mg/mL
• PKA: 14.18±0.10(Predicted)
• CAS DataBase Reference: PF03716556(CAS DataBase Reference)
• NIST Chemistry Reference: PF03716556(928774-43-0)
• EPA Substance Registry System: PF03716556(928774-43-0)

Safety Data

• WGK Germany: 3
• Hazardous Substances Data: 928774-43-0(Hazardous Substances Data)

Usage

Description

PF03716556 is a novel, potent, and selective acid pump antagonist that has been developed for the treatment of gastroesophageal reflux disease (GERD). It works by inhibiting the acid pump in the stomach, thereby reducing the amount of acid produced and alleviating the symptoms of GERD.

Uses

Used in Pharmaceutical Industry:
PF03716556 is used as a therapeutic agent for the treatment of gastroesophageal reflux disease. It is particularly effective in reducing the symptoms of GERD, such as heartburn and regurgitation, by inhibiting the acid pump in the stomach and decreasing the production of stomach acid. This selective and potent action makes PF03716556 a promising candidate for the management of GERD in patients who require long-term treatment or have not responded well to other treatments.

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.