AcebiluSTAT 是一种具有口服活性的白三烯 A4 水解酶抑制剂,可用于炎症研究。
产品描述
Acebilustat (ZK322) is an effective and specific leukotriene B4 hydrolase inhibitor.
体外活性
Acebilustat is a leukotriene A4 hydrolase inhibitor, which is safe and well tolerated in phase 1 trial[1]. Acebilustat is an antiinflammatory drug in development for the treatment of CF and other diseases. It is a potent inhibitor of the enzyme leukotriene A4 hydrolase (LTA4H), which catalyzes the rate-limiting step in the formation of leukotriene B4 (LTB4), a potent chemoattractant and activator of inflammatory immune cells including neutrophils[2].
激酶实验
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].
Cas No.
943764-99-6
分子式
C29H27N3O4
分子量
481.552
别名
阿西鲁司特;CTX-4430
储存和溶解度
Methanol:32 mg/mL
DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years