化合物ICI 118,551 hydrochloride T11607

Product Introduction
Bioactivity


英文名: ICI 118,551 hydrochloride

描述: ICI 118,551 hydrochloride (ICI 118551 hydrochloride) 是高度选择性的β2 adrenergic receptor 拮抗剂，能够结合 β2 肾上腺素能受体(Ki=0.7 nM)、β1 肾上腺素能受体 (Ki=49.5 nM) 和 β3 肾上腺素能受体 (Ki=611 nM)。

体外活性: ICI 118551 (10 μM) induces a prominent vasorelaxation of norepinephrine (NE)-precontracted PA but not AO [2]. ICI 118551 inhibits cAMP accumulation in IMCD cells (IC50: 1.7 μM) [1]. In the 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 the negative inotropic effects of ICI 118551 [3].

体内活性: ICI 118551 (0.2 mg/kg) injected into the jugular vein of the mice, strongly reduces systolic pressure in the pulmonary circuit but not systemic arterial pressure in vivo[2].

存储条件: store at low temperaturePowder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 20 mg/mL (63.72 mM)
H2O : 11 mg/mL (35.05 mM)


关键字: ICI118551 | ICI 118,551 hydrochloride | ICI 118551 | Adrenergic Receptor | ICI-118551 | ICI 118,551 Hydrochloride | Inhibitor | Beta Receptor | inhibit | ICI-118551 Hydrochloride | ICI 118,551 | ICI 118551 Hydrochloride | ICI118551 Hydrochloride

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相关库: Neurotransmitter Receptor Compound Library | Anti-Cancer Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Neuronal Signaling Compound Library | Inhibitor Library | GPCR Compound Library | Highly Selective Inhibitor Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途