MilliporeSigma™ Calbiochem™ Myeloperoxidase Inhibitor-II

Description

• A 5-fluorotryptamine derivative that inhibits myeloperoxidase/MPO activity (IC 50 = 18nM) via direct affinity interaction with enzyme active site heme pyrrole ring D, while exhibiting much reduced affinity toward serotonin reuptake transporter/SERT ( K i = 631nM)
• Kinetic studies reveal that the inhibitor acts as a good one-electron donor for the intermediate Compound I Fe(IV)=O...Por + , facilitating the formation of Compound II (Fe(IV)-OH...Por) and thereby preventing the reduction of Compound I directly to the resting state Fe(IV)...Por via the halogenation cycle, while, on the other hand, behaves as a poor electron donor for Compound II, thereby preventing the completion of the peroxidase cycle by stalling the further reduction of Compound II to the resting state
• Please note that the molecular weight for this compound is batch-specific due to variable water content.