PF-03716556

PF-03716556 is a potent, and selective acid pump antagonist for the treatment of gastroesophageal reflux disease. PF-03716556 demonstrated 3-fold greater inhibitory activity than revaprazan. PF-03716556 did not display any species differences, exhibiting highly selective profile including the canine kidney Na(+), K(+)-ATPase. Kinetics experiments revealed that PF-03716556 has a competitive and reversible mode of action.

Product information

CAS Number: 928774-43-0

Molecular Weight: 394.47

Formula: C22H26N4O3

Synonym:

PF 03716556

PF03716556

PF-3716556

PF 3716556

PF3716556

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

Smiles: CN(CCO)C(=O)C1C=C(N[C@@H]2CCOC3=CC=CC(C)=C32)C2=NC(C)=CN2C=1

InChiKey: YBHKBMJREUZHOV-QGZVFWFLSA-N

InChi: 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

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO: 79 mg/mL(200.26 mM). Water: Insoluble.

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

References:

1. Mori H, et al. J Pharmacol Exp Ther, 2009, 328(2), 671-679.

Products are for research use only. Not for human use.