| 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 | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 60 mg/mL (124.6 mM), Sonication is recommended.
Methanol : 32 mg/mL (66.45 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (2.08 mM), Sonication is recommended.
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| Keywords | LTB4 | Inhibitor | inhibit | CTX4430 | CTX 4430 | Aminopeptidase | Acebilustat |
| Inhibitors Related | Tosedostat | Montelukast sodium | L(+)-Leucinol | Pranlukast | Betulinic acid | Bestatin hydrochloride | Bestatin | Bufexamac | Tebufelone | LTβR-IN-1 | Ticolubant | SC-22716 |
| Related Compound Libraries | Nonsteroidal Anti-Inflammatory Compound Library | Bioactive Compound Library | ReFRAME Related Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Fibrosis Compound Library | Metabolism Compound Library | Immunology/Inflammation Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Human Metabolite Library | Coagulation and Anticoagulation Compound Library |
United States
