PF-06282999

PF-06282999 is an irreversible inhibitor of myeloperoxidase (MPO, Ki = 316.23 nM in a cell-free assay). It is selective for MPO over thyroid peroxidase (TPO) in a resorufin formation assay, as well as a panel of more than 50 enzymes, receptors, transporters, and ion channels at 100 µM. PF-06282999 inhibits MPO activity in isolated human whole blood with an IC50 value of 1.9 µM. It reduces the necrotic core area in atherosclerotic lesions by 37% in the aortic root of Ldlr-/- mice fed a Western diet when administered at a dose of 15 mg/kg twice per day for 14 weeks.Formal Name: 6-(5-chloro-2-methoxyphenyl)-3,4-dihydro-4-oxo-2-thioxo-1(2H)-pyrimidineacetamide. CAS Number: 1435467-37-0. Molecular Formula: C13H12ClN3O3S. Formula Weight: 325.8. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.50 mg/ml. lambdamax: 220, 276 nm. SMILES: O=C(C=C(C1=C(OC)C=CC(Cl)=C1)N2CC(N)=O)NC2=S. InChi Code: InChI=1S/C13H12ClN3O3S/c1-20-10-3-2-7(14)4-8(10)9-5-12(19)16-13(21)17(9)6-11(15)18/h2-5H,6H2,1H3,(H2,15,18)(H,16,19,21). InChi Key: ICYNYWFGIDGBRD-UHFFFAOYSA-N.