product name PF-3716556
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, it inhibits gastric acid secretion and displays no activity at Na+,K+-ATPase. PF-03716556 did not display any species differences, exhibiting highly selective profile including the canine kidney Na(+),K(+)-ATPase.
References: J Pharmacol Exp Ther. 2009 Feb;328(2):671-9.
394.47
Formula
C22H26N4O3
CAS No.
928774-43-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 79 mg/mL (200.3 mM)
Water: <1 mg/mL
Ethanol: 79 mg/mL (200.3 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19399806
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
| Animal model | Rat |
| Formulation & Dosage | Dissolved in 5% DMSO and 15% Cremophor EL; 1–10 mg/kg; 1 ml/kg; i.v. injection |
| References | J Pharmacol Exp Ther. 2009 Feb;328(2):671-9. |
Related Posts
product name PF-3716556
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, it inhibits gastric acid secretion and displays no activity at Na+,K+-ATPase. PF-03716556 did not display any species differences, exhibiting highly selective profile including the canine kidney Na(+),K(+)-ATPase.
References: J Pharmacol Exp Ther. 2009 Feb;328(2):671-9.
394.47
Formula
C22H26N4O3
CAS No.
928774-43-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 79 mg/mL (200.3 mM)
Water: <1 mg/mL
Ethanol: 79 mg/mL (200.3 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19399806
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
| Animal model | Rat |
| Formulation & Dosage | Dissolved in 5% DMSO and 15% Cremophor EL; 1–10 mg/kg; 1 ml/kg; i.v. injection |
| References | J Pharmacol Exp Ther. 2009 Feb;328(2):671-9. |