An irreversible MPO inhibitor (Ki = 316.23 nM in a cell-free assay); selective for MPO over TPO in a resorufin formation assay

PF-06282999 – 10 mg

Brand:
Cayman
CAS:
1435467-37-0
Storage:
-20
UN-No:
Non-Hazardous - /

PF-06282999 is an irreversible inhibitor of myeloperoxidase (MPO; Ki = 316.23 nM in a cell-free assay).{51086} 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.{48865}  

 

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SKU: 28406 - 10 mg Category:

Description

An irreversible MPO inhibitor (Ki = 316.23 nM in a cell-free assay); selective for MPO over TPO in a resorufin formation assay, as well as a panel of more than 50 enzymes, receptors, transporters, and ion channels at 100 µM; reduces necrotic core area in atherosclerotic lesions by 37% in the aortic root of Ldlr-/- mice fed a Western diet at 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

Synonyms: 

Molecular weight: 325.8

CAS: 1435467-37-0

Purity: ≥95%

Formulation: A crystalline solid

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