A myeloperoxidase inhibitor (Ki = 346.74 nM in a cell-free assay); selective for MPO over TPO and a panel of more than 50 enzymes

PF-1355 – 1 mg

Brand:
Cayman
CAS:
1435467-38-1
Storage:
-20
UN-No:
Non-Hazardous - /

PF-1355 is an irreversible myeloperoxidase (MPO) inhibitor (Ki = 346.74 nM in a cell-free assay).{51086} 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.{51087} 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.  

 

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Description

A myeloperoxidase inhibitor (Ki = 346.74 nM in a cell-free assay); selective for MPO over TPO and a panel of more than 50 enzymes, receptors, transporters, and ion channels; inhibits MPO activity in isolated human whole blood (IC50 = 1.5 µM); 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 BALF in a mouse model of pulmonary immune complex vasculitis at 20 and 100 mg/kg

Formal name: 6-(2,5-dimethoxyphenyl)-3,4-dihydro-4-oxo-2-thioxo-1(2H)-pyrimidineacetamide

Synonyms:  PF-06281355

Molecular weight: 321.4

CAS: 1435467-38-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ox Stress Reagents|Antioxidants||Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cardiovascular System|Cardiovascular Diseases||Research Area|Immunology & Inflammation|Autoimmunity||Research Area|Immunology & Inflammation|Innate Immunity

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