PF-3716556

Licensed and Manufactured by Pfizer Catalog No.S2222

PF-3716556 Chemical Structure

Molecular Weight(MW): 394.47

PF 3716556 is a potent and selective P-CAB (potassium-competitive acid blocker), with pIC50 of 6.026 and 7.095 for the inhibition of porcine H+,K+-ATPase activity in ion-leaky and ion-tight assay, respectively, inhibits gastric acid secretion, displays no activity at Na+,K+-ATPase, used for the treatment of gastroesophageal reflux disease.

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Biological Activity

Description PF 3716556 is a potent and selective P-CAB (potassium-competitive acid blocker), with pIC50 of 6.026 and 7.095 for the inhibition of porcine H+,K+-ATPase activity in ion-leaky and ion-tight assay, respectively, inhibits gastric acid secretion, displays no activity at Na+,K+-ATPase, used for the treatment of gastroesophageal reflux disease.
Targets
H+/K+-ATPase [1]
~6.5(pIC50)
In vitro

PF-03716556 is a potent, and selective acid pump antagonist with pIC50 of about of 6.026 and 7.095 for the inhibition of porcine H+,K+-ATPase activity in ion-leaky and ion-tight assay, respectively. PF-03716556 is used for the treatment of gastroesophageal reflux disease. PF-03716556 is highly selective for H+, K+-ATPase in vitro, displays no activity at Na+, K+-ATPase. PF-03716556 has no species differences among the porcine, canine and human enzymes. PF-03716556 has a competitive and reversible mode of action.[1]

In vivo PF-03716556 inhibits gastric acid secretion in rat and dog models. PF-03716556 offers long-lasting and maximal efficacy within 30 min of a single dosing with responses that are maintained for at least 5 days of repeated dosing with no signs of tolerance. [1]

Protocol

Animal Research:[1]
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  • Animal Models: rat
  • Formulation: 5% DMSO and 15% Cremophor EL
  • Dosages: 1–10 mg/kg; 1 ml/kg
  • Administration: i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 79 mg/mL (200.26 mM)
Ethanol 79 mg/mL (200.26 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 394.47
Formula

C22H26N4O3

CAS No. 928774-43-0
Storage powder
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID