PF-3716556

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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。

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
Formula	C22H26N4O3
CAS No.	928774-43-0
Storage	-20℃ for 3 years in powder form
Storage	-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 info	Chemical 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
Synonyms	PF-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 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	Rats
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.