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PF-3716556
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PF-3716556图片
CAS NO:928774-43-0
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
PF 3716556 (PF3716556; PF-3716556) is a novel, potent and selective P-CAB (potassium-competitive acid blocker: acid pump antagonist) with anti-acid reflux activity. It inhibits P-CAB 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. PF-3716556 inhibits gastric acid secretion and thus has the potential for the treatment of gastroesophageal reflux disease. It 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.
理化性质和储存条件
Molecular Weight (MW)394.47
FormulaC22H26N4O3
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)
Other infoChemical Name: 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
InChi Key: YBHKBMJREUZHOV-QGZVFWFLSA-N
InChi Code: InChI=1S/C22H26N4O3/c1-14-5-4-6-19-20(14)17(7-10-29-19)24-18-11-16(22(28)25(3)8-9-27)13-26-12-15(2)23-21(18)26/h4-6,11-13,17,24,27H,7-10H2,1-3H3/t17-/m1/s1
SMILES Code: O=C(C1=CN2C(C(N[C@@H]3CCOC4=C3C(C)=CC=C4)=C1)=NC(C)=C2)N(CCO)C
SynonymsPF-3716556; PF 3716556; PF3716556; PF-03716556; PF 03716556; PF03716556
实验参考方法
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: PF 03716556 is a potent, and selective H+, K+-ATPase antagonist, with a pIC50 value of 6.009.

In VivoPF-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 modelRats
Formulation & DosageDissolved in 5% DMSO and 15% Cremophor EL; 1–10 mg/kg; 1 ml/kg; i.v. injection
ReferencesJ Pharmacol Exp Ther. 2009 Feb;328(2):671-9.