For research use only. Not for therapeutic Use.
PF-1355 is a selective 2-thiouracil mechanism-based MPO inhibitor, used for treatment of vasculitic diseases.
In a dose-responsive fashion, PF-1355 inhibits MPO activity in phorbol ester-stimulated human neutrophils as measured by taurine chlorination (EC50=1.47 μM) as well as lipopolysaccharide-treated human blood measuring residual MPO activity (EC50=2.03 μM)[1].
Oral administration of PF-1355 reduces plasma MPO activity, vascular edema, neutrophil recruitment, and elevates circulating cytokines. In a model of anti-glomerular basement membrane disease, formerly known as Goodpasture disease, albuminuria and chronic renal dysfunction are completely suppressed by PF-1355 treatment[1].
Catalog Number | I001680 |
CAS Number | 1435467-38-1 |
Synonyms | 2-[6-(2,5-dimethoxyphenyl)-4-oxo-2-sulfanylidenepyrimidin-1-yl]acetamide |
Molecular Formula | C14H15N3O4S |
Purity | ≥95% |
InChI | InChI=1S/C14H15N3O4S/c1-20-8-3-4-11(21-2)9(5-8)10-6-13(19)16-14(22)17(10)7-12(15)18/h3-6H,7H2,1-2H3,(H2,15,18)(H,16,19,22) |
InChIKey | LJBUZOGABRDGBR-UHFFFAOYSA-N |
SMILES | COC1=CC(=C(C=C1)OC)C2=CC(=O)NC(=S)N2CC(=O)N |
Reference | [1]. Zheng W, et al. PF-1355, a mechanism-based myeloperoxidase inhibitor, prevents immune complex vasculitis and anti-glomerular basement membrane glomerulonephritis. J Pharmacol Exp Ther. 2015 May;353(2):288-98 |