PF 03716556
Based on 1 Customer Validation
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.
- Purity: 99.10%
- CAS No.: 928774-43-0
- Formula: C22H26N4O3
- Molecular Weight:394.47
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Biological Activity
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 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats (250 -300 g) treated with Pentagastrin[1]
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Dosage:1 mg/kg, 3 mg/kg, 10 mg/kg
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Administration:Intraduodenal administration; once
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Result:Inhibited gastric acid secretion in a dose-dependent manner.
Chemical Information
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CAS No. 928774-43-0
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Appearance Solid
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Molecular Weight 394.47
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Formula C22H26N4O3
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Color White to yellow
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SMILES
CC1=CN2C=C(C=C(C2=N1)N[C@H]3C4=C(C=CC=C4OCC3)C)C(N(CCO)C)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
DMSO : 23 mg/mL (58.31 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Hiroki Mori, et al. 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 Feb;328(2):671-9. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5350 mL | 12.6752 mL | 25.3505 mL | 63.3762 mL |
| 5 mM | 0.5070 mL | 2.5350 mL | 5.0701 mL | 12.6752 mL | |
| 10 mM | 0.2535 mL | 1.2675 mL | 2.5350 mL | 6.3376 mL | |
| 15 mM | 0.1690 mL | 0.8450 mL | 1.6900 mL | 4.2251 mL | |
| 20 mM | 0.1268 mL | 0.6338 mL | 1.2675 mL | 3.1688 mL | |
| 25 mM | 0.1014 mL | 0.5070 mL | 1.0140 mL | 2.5350 mL | |
| 30 mM | 0.0845 mL | 0.4225 mL | 0.8450 mL | 2.1125 mL | |
| 40 mM | 0.0634 mL | 0.3169 mL | 0.6338 mL | 1.5844 mL | |
| 50 mM | 0.0507 mL | 0.2535 mL | 0.5070 mL | 1.2675 mL |