A myeloperoxidase inhibitor
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PF-1355

Item No. 22222

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-(2,5-dimethoxyphenyl)-3,4-dihydro-4-oxo-2-thioxo-1(2H)-pyrimidineacetamide
CAS Number
1435467-38-1
Synonyms
  • PF-06281355
Molecular Formula
C14H15N3O4S
Formula Weight
321.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMF:PBS (pH 7.2) (1:1): 0.5 mg/mlDMSO: 10 mg/mlEthanol: 5 mg/ml
λmax
221, 275 nm
SMILES
COC1=CC(C(N(CC(N)=O)C(N2)=S)=CC2=O)=C(OC)C=C1
InChi Code
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)
InChi Key
LJBUZOGABRDGBR-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Cayman Chemical
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    Product Description

    PF-1355 is an irreversible myeloperoxidase (MPO) inhibitor (Ki = 346.74 nM in a cell-free assay).1 It is selective for MPO over thyroid peroxidase (TPO) and over a panel of more than 50 enzymes, receptors, transporters, and ion channels. It inhibits MPO activity in isolated human whole blood with an IC50 value of 1.5 µM. PF-1355 reduces MPO activity in plasma and peritoneal lavage fluid in a mouse model of peritonitis.2 It also reduces lung edema, decreases plasma levels of TNF-α, MCP-1/CCL2, MIP-2/CXCL2, and KC/CXCL1 and transiently increases and then reduces neutrophil levels in bronchoalveolar lavage fluid (BALF) in a mouse model of pulmonary immune complex vasculitis when administered at doses of 20 and 100 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ruggeri, R.B., Buckbinder, L., Bagley, S.W., et al. 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(21), 8513-8523 (2015).

    2. Zheng, W., Warner, R., Ruggeri, R., et al. PF-1355, a mechanism-based myeloperoxidase inhibitor, prevents immune complex vasculitis and anti-glomerular basement membrane glomerulonephritis. J. Pharmacol. Exp. Ther. 353(2), 288-298 (2015).