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72795-01-8

中文名称 ICI 118,551 HYDROCHLORIDE
英文名称 (±)-erythro-(S*,S*)-1-[2,3-(Dihydro-7-methyl-1H-inden-4-yl)oxy]-3-[(1-methylethyl)amino]-2-butanolhydrochloride
CAS 72795-01-8
分子式 C17H28ClNO2
分子量 313.863
MOL 文件 72795-01-8.mol
更新日期 2024/05/22 15:59:43
72795-01-8 结构式 72795-01-8 结构式

基本信息

中文别名
ICI 118551 盐酸盐
英文别名
CS-769
CI 118551 Hydrochloride
ICI 118,551 hydrochloride, >=98%
(2R,3R)-rel-1-[(2,3-Dihydro-7-methyl-1H-inden-4-yl)oxy]-3-[(1-methylethyl)amino]-2-butanol hydrochloride (1:1)
(±)-erythro-(S*,S*)-1-[2,3-(Dihydro-7-methyl-1H-inden-4-yl)oxy]-3-[(1-methylethyl)amino]-2-butanolhydrochloride

物理化学性质

储存条件desiccated
溶解度DMSO : 25 mg/mL (79.65 mM; Need ultrasonic)H2O : 12.5 mg/mL (39.83 mM; Need ultrasonic)
形态粉末
颜色白色

安全数据

WGK Germany3
ICI 118,551 HYDROCHLORIDE价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2024/04/30S8114ICI 118,551 HYDROCHLORIDE
ICI-118551 Hydrochloride
72795-01-85mg1613.61元
2024/04/30S8114Zenidolol (ICI-118551) Hydrochloride72795-01-810mM (1mL in DMSO)1875.51元
2024/04/30S8114ICI 118,551 HYDROCHLORIDE
ICI-118551 Hydrochloride
72795-01-825mg4889.65元

常见问题列表

生物活性
ICI 118,551 hydrochloride 是一种高度选择性的 β2 adrenergic receptor 拮抗剂,结合 β2,β1 和 β3 肾上腺素能受体的Ki 值分别为 0.7,49.5 和 611 nM。
靶点

Ki: 0.7nM (β2 receptor), 49.5 nM (β1 receptor), 611 nM (β3 receptor)

体外研究

ICI 118551 inhibits cAMP accumulation with IC 50 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.

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.

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