PF 06281355

Cat. No. 6004

PF 06281355 C14H15N3O4S [1435467-38-1]

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Chemical Name: 6-(2,5-Dimethoxyphenyl)-3,4-dihydro-4-oxo-2-thioxo-1(2H)-pyrimidineacetamide

Biological Activity

Selective myeloperoxidase (MPO) inhibitor (IC50 = 1.5 μM in LPS-stimulated human whole blood). Selective for MPO over a panel of 50 receptors, enzymes, ion channels and transporters, including thyroid peroxidase. Inhibits MPO activity in peritoneal lavage and plasma in a murine peritonitis model. Also reduces lung edema in a murine pulmonary immune complex vasculitis model. Orally bioavailable.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc

Technical Data

M.Wt:
321.35
Formula:
C14H15N3O4S
Solubility:
Soluble to 20 mM in DMSO with gentle warming
Purity:
>98 %
Storage:
Store at RT
CAS No:
1435467-38-1

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Ruggeri et al (2015) Discovery of 2-(6-(5-chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999): A highly selective mechanism-based myeloperoxidase inhibitor for the treatment of cardiovascular diseases. J.Med.Chem. 58 8513. PMID: 26509551 .

Zheng et al (2015) PF-1355, a mechanism-based myeloperoxidase inhibitor, prevents immune complex vasculitis and anti-glomerular basement membrane glomerulonephritis. J.Pharmacol.Exp.Ther. 353 288. PMID: 25698787 .

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Keywords: PF 06281355, supplier, PF06281355, myeloperoxidase, inhibitors, inhibits, selective, orally, bioavailable, vasculitis, Tocris Bioscience, Other Oxygenase/Oxidase Inhibitor products

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