PXS-4681A is a powerful, specific, and irreversible inhibitor of semicarbazide-sensitive amine oxidase (SSAO; VAP-1), with an oral activity and a Ki value of 37 nM. It exhibits exceptional selectivity towards related amine oxidases, ion channels, and seven-transmembrane domain receptors. Additionally, PXS-4681A demonstrates potent anti-inflammatory properties.

SSAO:37 nM (Ki)

PXS-4681A effectively inhibits the enzyme SSAO/VAP-1 across multiple species including humans, rats, mice, rabbits, and dogs, demonstrating potent activity with IC50 values of 3 nM, 3 nM, 2 nM, 9 nM, and 3 nM, respectively[1].

PXS-4681A (2 mg/kg; PO; single dose) effectively reduces neutrophil migration, tumor necrosis factor-α, and interleukin-6 levels in mouse models of lung and localized inflammation[1]. It exhibits excellent absorption, bioavailability, and oral half-life, showing promise in rats at 10 mg/kg IV and 20 mg/kg oral doses, and in BALB/C mice at 2 mg/kg for both administration routes[1]. In Carrageenan-induced skin inflammation in animals, a single 2 mg/kg oral dose significantly decreased local inflammation, reducing exudate volume by 25%[1].