ICI 118,551 hydrochloride

ICI 118,551 hydrochlorideCAS号: 72795-01-8分子式: C17H27NO2.HCl分子量: 313.87描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述

ICI 118,551 (hydrochloride) is a highly selective β2 adrenergic receptor antagonist, with Kis of 0.7, 49.5 and 611 nM for β2, β1 and β3 receptors, 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
ICI 118551 hydrochloride
外观
white powder
可溶性/溶解性
DMSO : 25 mg/mL (79.65 mM; Need ultrasonic)
H2O : 12.5 mg/mL (39.83 mM; Need ultrasonic)
生物活性
靶点
β2 receptor,β1 receptor,β3 receptor
In vitro(体外研究)
ICI 118551 inhibits cAMP accumulation with IC50 of 1.7 μM in IMCD cells. ICI 118551 (10 μM) induces a prominent vasorelaxation of norepinephrine (NE)-precontracted PA but not AO. In failing human heart, ICI 118551 has significant effects on beat duration, with time-to-peak contraction and time-to-90% relaxation reduced compared with basal contraction. Negative Inotropic Effect of ICI 118551 Is Not cAMP-Related. Overexpression of β2AR in rabbit myocytes enhances negative inotropic effects of ICI 118551.
In vivo(体内研究)
ICI 118551 (0.2 mg/kg) injected into the jugular vein of the mice, reduces systolic pressure in the pulmonary circuit but not systemic arterial pressure.

分子结构图

ICI 118,551 hydrochloride