Acebilustat (CTX-4430) (ZK322) is an effective and specific leukotriene B4 hydrolase inhibitor.

Acebilustat, a potent leukotriene A4 hydrolase (LTA4H) inhibitor, demonstrated safety and tolerability in a phase 1 trial[1]. Currently under development as an anti-inflammatory medication, it targets CF among other diseases by inhibiting LTA4H, the crucial enzyme in leukotriene B4 (LTB4) production. LTB4 acts as a powerful chemoattractant and activator for inflammatory immune cells, such as neutrophils[2], thus Acebilustat's mechanism holds promise for mitigating inflammatory responses.

Rolapitant is made at a stock concentration of 1 mM in 100% DMSO. For most receptor binding studies, the stock solution is diluted with the final concentrations ranged from 0.1 to 3 μM. Radioligand concentrations for competition binding studies ranged from 0.5 to 1 nM. For species comparison studies, 150 pM [125I]-BHSP is incubated with varying concentrations of protein (10-50 μg) prepared from gerbil, rabbit and monkey striata, and from cells expressing cloned rat, mouse and guinea pig NK receptors[1].