Name | Acebilustat |
Description | Acebilustat (CTX-4430) (ZK322) is an effective and specific leukotriene B4 hydrolase inhibitor. |
Kinase Assay | 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]. |
In vitro | 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. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 60 mg/mL (124.69 mM) Methanol : 32 mg/mL
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Keywords | CTX 4430 | Aminopeptidase | Inhibitor | inhibit | CTX4430 | Acebilustat |
Inhibitors Related | Montelukast sodium | Bestatin hydrochloride | Bestatin |
Related Compound Libraries | Nonsteroidal Anti-Inflammatory Compound Library | Bioactive Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Orally Active Compound Library | Metabolism Compound Library | Bioactive Compounds Library Max | Coagulation and Anticoagulation Compound Library |