ORM-15341 is a potent and full antagonist for human AR (hAR) with IC50 values of 38 nM as shown by transactivation assays in AR-HEK293 cells stably expressing full-length hAR and an androgen-responsive luciferase reporter gene construct.IC50 value: 38 nMTarget: androgen receptor in vitro: In competitive AR binding assays, the inhibition constant (Ki) values of ORM-15341 was 8 nM. ORM-15341 functions as a full antagonist for all tested mutant ARs , with IC50 of 25, 51, 700, and 1160 nM for wtAR, AR(F876L), AR(T877A), and AR(W741L).
规格
规格或纯度
10mM in DMSO
英文名称
ORM-15341
生化机理
在稳定表达全长 hAR 和雄激素反应型荧光素酶报告基因构建体的 AR-HEK293 细胞中进行的转录激活试验表明,ORM-15341 是一种强效的人 AR(hAR)完全拮抗剂,其 IC50 值为 38 nM:38 n