Amelubant (BIIL 284) is a potent, oral and long acting LTB 4 receptor antagonist, negligibly binds to LTB 4 receptor, with K i s of 221 nM and 230 nM in vital cells and membranes. Amelubant (BIIL 284) is a prodrug of active metabolites BIIL 260 and BIIL 315. Anti-inflammatory activity.
性状
Solid
IC50 & Target[1][2]
LTB4 221 nM (Ki, in vital human granulocytes) LTB4
体外研究(In Vitro)
Amelubant is a prodrug of active metabolites BIIL 260 and BIIL 315, which are reversible and competitive LTB4 receptor antagonists, with Kis of 1.4, 1.1 nM and 1.7, 1.9 nM in vital cells and membranes, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Birke FW, et al. In vitro and in vivo pharmacological characterization of BIIL 284, a novel and potent leukotriene B(4) receptor antagonist. J Pharmacol Exp Ther. 2001 Apr;297(1):458-66.
溶解度数据
In Vitro: DMSO : 100 mg/mL (185.66 mM; Need ultrasonic)配制储备液