Cas No.: | 1435467-38-1 |
Chemical Name: | 1(2H)-Pyrimidineacetamide, 6-(2,5-dimethoxyphenyl)-3,4-dihydro-4-oxo-2-thioxo- |
Synonyms: | PF06281355;PF1355;PF 1355;PF-06281355;PF 06281355 |
SMILES: | O=C(CN1C(=CC(=O)NC1=S)C1C(OC)=CC=C(OC)C=1)N |
Formula: | C14H15N3O4S |
M.Wt: | 321.3516 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | PF-1355 is a selective 2-thiouracil mechanism-based MPO inhibitor, used for treatment of vasculitic diseases. |
In Vivo: | 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]. |
In Vitro: | 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]. |