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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.
Sold for research purposes under agreement from Pfizer Inc
|Storage||Store at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|DMSO||6.43||20 with gentle warming|
Preparing Stock Solutions
The following data is based on the product molecular weight 321.35. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.2 mM||15.56 mL||77.8 mL||155.59 mL|
|1 mM||3.11 mL||15.56 mL||31.12 mL|
|2 mM||1.56 mL||7.78 mL||15.56 mL|
|10 mM||0.31 mL||1.56 mL||3.11 mL|
References are publications that support the biological activity of the product.
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
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
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Keywords: PF 06281355, PF 06281355 supplier, PF06281355, myeloperoxidase, inhibitors, inhibits, selective, orally, bioavailable, vasculitis, Other, Oxygenases/Oxidases, 6004, Tocris Bioscience
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