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PF03716556

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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
Product Categories:
  • Amines
  • Aromatics
  • Heterocycles
  • Inhibitors
  • Intermediates & Fine Chemicals
  • Pfizer Compounds
  • Pharmaceuticals
Mol File:
928774-43-0.mol
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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
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Safety Information

WGK Germany 
3
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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.

storage

-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.

PF03716556Supplier

Shanghai Boyle Chemical Co., Ltd.
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Email
sales@boylechem.com
J & K SCIENTIFIC LTD.
Tel
010-82848833 400-666-7788
Email
jkinfo@jkchemical.com
Chemsky(shanghai)International Co.,Ltd.
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021-50135380
Email
shchemsky@sina.com
China DongFan Chemical Co.,LTD
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86-0571-85151182
Dalian Meilun Biotech Co., Ltd.
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0411-62910999 13889544652
Email
sales@meilune.com
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