PF 3716556

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Cat.No. 4191 - PF 3716556 | C22H26N4O3 | CAS No. 928774-43-0
Description: Selective H+,K+-ATPase inhibitor
Chemical Name: 8-[[(4R)-3,4-Dihydro-5-methyl-2H-1-benzopyran-4-yl]amino]-N-(2-hydroxyethyl)-N,2-dimethyl-imidazo[1,2-a]pyridine-6-carboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

H+,K+-ATPase inhibitor (pIC50 = 6 in human recombinant ion-leaky assays); more potent in acidic conditions. Highly selective for H+,K+-ATPase in vitro; displays no activity at Na+,K+-ATPase. Also displays selectivity for H+,K+-ATPase over a range of 50 receptors and ion channels (IC50 > 10 μM). Inhibits gastric acid secretion in rat and dog models.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data

M. Wt 394.47
Formula C22H26N4O3
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 928774-43-0
PubChem ID 25134521
InChI Key YBHKBMJREUZHOV-QGZVFWFLSA-N
Smiles OCCN(C)C(C2=CN1C(C(N[C@H]4C3=C(C)C=CC=C3OCC4)=C2)=NC(C)=C1)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 39.45 100

Preparing Stock Solutions

The following data is based on the product molecular weight 394.47. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.54 mL 12.68 mL 25.35 mL
5 mM 0.51 mL 2.54 mL 5.07 mL
10 mM 0.25 mL 1.27 mL 2.54 mL
50 mM 0.05 mL 0.25 mL 0.51 mL

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References

References are publications that support the biological activity of the product.

Mori et al (2009) 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 (PF-03716556), a novel, potent, and selective acid pump antagonist for the treatment of gastroesop J.Pharmacol.Exp.Ther. 328 671 PMID: 18981288


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Citations for PF 3716556

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