1. Membrane Transporter/Ion Channel
  2. Proton Pump
  3. PF 03716556

PF 03716556 

Cat. No.: HY-13100
Handling Instructions

PF 03716556 is a potent, selective, competitive and reversible acid pump (H+,K+-ATPase) antagonist with pIC50s of 6.026, 6.038 and 6.009 for porcine, canine, and human recombinant gastric H+,K+-ATPase, respectively. PF 03716556 is inactive against other receptors, ion channels, and enzymes. PF 03716556 has the potential for gastroesophageal reflux disease research.

For research use only. We do not sell to patients.

PF 03716556 Chemical Structure

PF 03716556 Chemical Structure

CAS No. : 928774-43-0

Size Stock
10 mM * 1  mL in DMSO Get quote
10 mg USD 108 Get quote
25 mg USD 216 Get quote
50 mg USD 408 Get quote
100 mg USD 768 Get quote

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Description

PF 03716556 is a potent, selective, competitive and reversible acid pump (H+,K+-ATPase) antagonist with pIC50s of 6.026, 6.038 and 6.009 for porcine, canine, and human recombinant gastric H+,K+-ATPase, respectively. PF 03716556 is inactive against other receptors, ion channels, and enzymes. PF 03716556 has the potential for gastroesophageal reflux disease research[1].

IC50 & Target

pIC50: 6.026 (Porcine gastric H+,K+-ATPase), 6.038 (Canine gastric H+,K+-ATPase) and 6.009 (Recombinant gastric H+,K+-ATPase)[1]

In Vitro

In porcine ion-tight membrane vesicles, PF 03716556 inhibits H+,K+-ATPase activity in a concentration-dependent manner, with a pIC50 value of 7.095 at pH 7.4[1].

In Vivo

PF 03716556 (1-10 mg/kg; intraduodenal administration; once; male Sprague-Dawley rats) treatment inhibits gastric acid secretion in a dose-dependent manner in rats[1].

Animal Model: Male Sprague-Dawley rats (250 -300 g) treated with Pentagastrin[1]
Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg
Administration: Intraduodenal administration; once
Result: Inhibited gastric acid secretion in a dose-dependent manner.
Molecular Weight

394.47

Formula

C₂₂H₂₆N₄O₃

CAS No.

928774-43-0

SMILES

CC1=CN2C=C(C=C(C2=N1)N[[email protected]]3C4=C(C=CC=C4OCC3)C)C(N(CCO)C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 23 mg/mL (58.31 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5350 mL 12.6752 mL 25.3505 mL
5 mM 0.5070 mL 2.5350 mL 5.0701 mL
10 mM 0.2535 mL 1.2675 mL 2.5350 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

PF 03716556PF03716556PF-03716556Proton PumpAcidpumpH+,K+-ATPasesecretiongastroesophagealrefluxInhibitorinhibitorinhibit

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PF 03716556
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