LCI-699

LCI-699CAS号: 928134-65-0分子式: C13H10FN3分子量: 227.241描述纯度储存/保存方法别名可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述
silodrostat is a potent inhibitor of human 11β-hydroxylase and aldosterone synthase with IC50 values of 2.5 and 0.7 nM, respectively.
纯度
>98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
别名
LCI-699;LCI699
可溶性/溶解性
DMSO : 250 mg/mL (1100.16 mM; Need ultrasonic)
Ethanol : 100 mg/mL (440.06 mM; Need ultrasonic)
生物活性
靶点
11β-hydroxylase
In vitro(体外研究)
LCI699 also inhibits aldosterone synthase (CYP11B2) other than CYP11B1.
In vivo(体内研究)
LCI699 is a potent inhibitor of 11β-hydroxylase (CYP11B1), the enzyme that catalyzes the final step of cortisol synthesis, and has a half-life of ∼4 hours. It decreases blood pressure (BP) in patients with essential hypertension and primary aldosteronism. Treatment with LCI699 is well tolerated, it is demonstrated efficacy with a satisfactory safety and tolerability profile in the proof-of-concept study in Cushing’s disease. The administration of LCI699, up to 1.0 mg BID, effectively and safely inhibits aldosterone synthase in patients with primary aldosteronism.

分子结构图

LCI-699