Product Description
ICI 118,551 (hydrochloride) is a highly selective β2 adrenergic receptor antagonist, with Ki values of 0.7, 49.5 and 611 nM for β2, β1 and β3 receptors, respectively.
IC50 & Target: Ki: 0.7nM (β2 receptor), 49.5 nM (β1 receptor), 611 nM (β3 receptor)
In Vitro: ICI 118551 inhibits cAMP accumulation with IC50 of 1.7 μM in IMCD cells[1]. ICI 118551 (10 μM) induces a prominent vasorelaxation of norepinephrine (NE)-precontracted PA but not AO[2]. 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[3].
In Vivo: 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[2].
Information
CAS No72795-01-8
FormulaC17H28ClNO2
Clinical Informationclinicalinformation
PathwayGPCR/G Protein
Neuronal Signaling
TargetAdrenergic Receptor
Specifications
FormWhite to off-white (Solid)
Purity / Grade99.76%
SolubilityH2O : 12.5 mg/mL (39.83 mM; Need ultrasonic)
DMSO : 33.33 mg/mL (106.19 mM; Need ultrasonic)
SmilesCC1=C(CCC2)C2=C(OC[C@H](O)[C@@H](C)NC(C)C)C=C1.[H]Cl
Misc Information
Storage Instruction2-8°C, sealed storage, away from moisture
Alternative NamesICI 118551 hydrochloride; 2-Butanol, 1-[(2,3-dihydro-7-methyl-1H-inden-4-yl)oxy]-3-[(1-methylethyl)amino]-, hydrochloride(1:1), (2R,3R)-rel
Observed Molecular Weight313.86
References[1]. Yasuda G, et al. The beta 1- and beta 2-adrenoceptor subtypes in cultured rat inner medullary collecting duct cells. Am J Physiol. 1996 Sep;271(3 Pt
2):F762-9.
[2]. Wenzel D, et al. beta(2)-adrenoceptor antagonist ICI 118,551 decreases pulmonary vascular tone in mice via a G(i/o) protein/nitric oxide-coupled
pathway. Hypertension. 2009 Jul;54(1):157-63.
[3]. Gong H, et al. Specific beta(2)AR blocker ICI 118,551 actively decreases contraction through a G(i)-coupled form of the beta(2)AR in myocytes from
failing human heart. Circulation. 2002 May 28;105(21):2497-503.
[4]. Hoffmann C, et al. Comparative pharmacology of human beta-adrenergic receptor subtypes--characterization of stably transfected receptors in CHO
cells. Naunyn Schmiedebergs Arch Pharmacol. 2004 Feb;369(2):151-9.