Uses
(S)-3-((Tetrahydrofuran-2-yl)methyl)-2-thioxo-1,2,3,7-tetrahydro-6H-purin-6-one is used as an internal standard and also as an analytical standard.
Biological Activity
AZD5904 (TX4) is an orally active 2-thioxanthine class suicide substrate th at targets myeloperoxidase (MPO) for mechanism-based inactivation, covalently modifying MPO heme group without converting the enzyme to compound II. AZD5904 effectively inhibits peroxide-induced human MPO chlorination activity (IC50 = 0.2 μM) and extracellular MPO activity in PMA-stimulated human neutrophil cultures (by 68% at 1 μM). Oral administration (20-180 μmol/kg) of the racemate (TX3) is efficacious in reducing inflammation site MPO activity in mice in vivo with 10- to 19-fold selectivity over lactoperoxidase (LPO), thyroid peroxidase (TPO), and >70-fold selectivity over a panel of other enzymes, ion channels, and receptors.
