PF 06281355

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Cat.No. 6004 - PF 06281355 | C14H15N3O4S | CAS No. 1435467-38-1
Description: Selective myeloperoxidase (MPO) inhibitor
Chemical Name: 6-(2,5-Dimethoxyphenyl)-3,4-dihydro-4-oxo-2-thioxo-1(2H)-pyrimidineacetamide
Purity: ≥98% (HPLC)
Datasheet
Citations
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Literature

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
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 1435467-38-1
PubChem ID 71568997
InChI Key LJBUZOGABRDGBR-UHFFFAOYSA-N
Smiles COC1=CC(C2=CC(NC(N2CC(N)=O)=S)=O)=C(C=C1)OC

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 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 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 3.11 mL 15.56 mL 31.12 mL
5 mM 0.62 mL 3.11 mL 6.22 mL
10 mM 0.31 mL 1.56 mL 3.11 mL
50 mM 0.06 mL 0.31 mL 0.62 mL

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Product Datasheets

Safety Datasheet

References

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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Literature in this Area

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