A 5-fluorotryptamine derivative that inhibits myeloperoxidase/MPO activity (IC50 = 18nM) via direct affinity interaction with enzyme active site heme pyrrole ring D, while exhibiting much reduced affinity toward serotonin reuptake transporter/SERT (Ki = 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. Alternate Names: 4-(5-Fluoro-1H-indol-3-yl)butanamide, MPO Inhibitor II Molecular Formula: C12H13FN2O Primary Target: Myeloperoxidase Solubility: DMSO Storage and Stability: Store at 4C under inert atmosphere. For maximum recovery of product, centrifuge the original vial prior to removing the cap.
Purity:
95% (HPLC)
Form:
Supplied as a light beige powder.
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