A myeloperoxidase inhibitor
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PF-06282999

Item No. 28406

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.50 mg/ml
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $49

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    5 mg

    $107

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    10 mg

    $190

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    25 mg

    $412

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    Product Description

    PF-06282999 is an irreversible inhibitor of myeloperoxidase (MPO; Ki = 316.23 nM in a cell-free assay).1 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.2

    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. Roth Flach, R.J., Su, C., Bollinger, E., et al. Myeloperoxidase inhibition in mice alters atherosclerotic lesion composition. PLoS One 14(3), e0214150 (2019).