[CAS NO. 928774-43-0] PF-3716556
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PRODUCTS SPECIFICATIONS [928774-43-0]
Store
Catalog
SLK-S2222
Brand
Selleck
CAS
928774-43-0
DESCRIPTION [928774-43-0]
Overview
| MDL | MFCD19690947 |
|---|---|
| Molecular Weight | 394.47 |
| Molecular Formula | C22H26N4O3 |
| SMILES | O=C(C1=CN2C(C(N[C@@H]3CCOC4=C3C(C)=CC=C4)=C1)=NC(C)=C2)N(CCO)C |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 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 |
| 50 mM | 0.0507 mL | 0.2535 mL | 0.5070 mL |
Description
PF 3716556 is a potent and selective (potassium-competitive acid blocker), with of 6.026 and 7.095 for the inhibition of porcine 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.
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.
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