PXS-4681A

PXS-4681A is a potent, selective, irreversible and orally active semicarbazide-sensitive amine oxidase (SSAO; VAP-1) inhibitor with a K_i of 37 nM. PXS-4681A shows highly selectivity over related amine oxidases, ion channels, and seven-transmembrane domain receptors. PXS-4681A has anti-inflammatory effects^[1]. IC50 & Target: Ki: 37 nM (SSAO)^[1] In Vitro: PXS-4681A is an inhibitor of SSAO/VAP-1 in human, rat, mouse, rabbit, and dog species with IC₅₀ values of 3 nM, 3 nM, 2 nM, 9 nM and 3nM, respectively^[1]. In Vivo: PXS-4681A (2 mg/kg; PO; single dose) attenuates neutrophil migration, tumor necrosis factor-α, and interleukin-6 levels in mouse models of lung inflammation and localized inflammation^[1].
In rats, PXS-4681A is well absorbed with good bioavailability and oral half-life at the 10 mg/kg i.v. dose and the 20 mg/kg PO dose. Similarly, in BALB/C mice, PXS-4681A is well absorbed with good bioavailability and oral half-life at 2 mg/kg in both intravenous and oral studies^[1].