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(RS)-ICI-118551 Hydrochloride

Catalog No. T6860Cas No. 1217094-53-5
Alias ICI-118,551

ICI-118551 Hydrochloride (ICI-118,551) 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.

(RS)-ICI-118551 Hydrochloride

(RS)-ICI-118551 Hydrochloride

Purity: 98.02%
Catalog No. T6860Alias ICI-118,551Cas No. 1217094-53-5
ICI-118551 Hydrochloride (ICI-118,551) 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.
Pack SizePriceAvailabilityQuantity
1 mg$195In Stock
5 mg$483In Stock
10 mg$692In Stock
25 mg$1,080In Stock
50 mg$1,490In Stock
100 mg$1,970In Stock
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Purity:98.02%
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Product Introduction

Bioactivity
Description
ICI-118551 Hydrochloride (ICI-118,551) 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.
Targets&IC50
β3-adrenoceptor:611nM(Ki), β2-adrenoceptor:0.7nM(Ki), β1-adrenoceptor:49.5nM(Ki)
In vitro
ICI-118551 inhibits cAMP accumulation by 50% (IC50 = 1.7 mM)[1]. Pharmacological experiments proves that the right shift of the norepinephrine dose-response curve by ICI 118551 is mediated via a beta(2)-adrenoceptor/G(i/o) protein-dependent pathway enhancing NO production in the endothelium; these results are corroborated in beta-adrenoceptor and endothelial NO synthase knockout mice where ICI 118551 has no effect. ICI 118551 increases vascular lumen diameter in lung sections and reduces pulmonary arterial pressure under normoxia and under hypoxia in the isolated perfused lung model[2]. Transgenic mice with high beta(2)AR number and increased G(i) levels have normal basal contractility but show a similar negative inotropic response to ICI 118,551. Overexpression of human beta(2)AR in rabbit myocytes using adenovirus potentiates the negative inotropic effect of ICI 118,551. In human, rabbit, and mouse myocytes, the negative inotropic effects are blocked after treatment of cells with pertussis toxin to inactivate G(i), and overexpression of G(i)alpha(2) induces the effect de novo in normal rat myocytes[5].
In vivo
After 1 week of treatment, ICI 118,551 has no effect on the beta 1-receptor mediated shortening of electromechanical systole (QS2I), the rise in systolic pressure and rise in renin, whereas these responses are blocked by a dose factor of eight after propranolol. ICI 118,551 and propranolol equally block the beta 2-receptor mediated fall in diastolic pressure and the rise in noradrenaline. beta 2-selective blockade by ICI 118,551 lowers blood pressure[4].
Cell Research
Binding reactions are carried out by incubating 60 μg of membranes with 10 nM [3H]dihydroalprenolol hydrochloride and different concentrations of ICI 118,551. After a two hour incubation at room-temperature, the binding reactions are terminated by rapid filtration over glass fiber filters. Radioactivity in the filters is then quantified using a liquid scintillation counter. Non-specific binding is determined in the presence of 1 μM alprenolol. Binding data are analyzed with GraphPad Prism software. (Only for Reference)
AliasICI-118,551
Chemical Properties
Molecular Weight313.86
FormulaC17H27NO2·HCl
Cas No.1217094-53-5
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
Ethanol: 27 mg/mL (86 mM)
H2O: 19 mg/mL (60.5 mM)
DMSO: 58 mg/mL (184.8 mM)
Solution Preparation Table
H2O/Ethanol/DMSO
1mg5mg10mg50mg
1 mM3.1861 mL15.9307 mL31.8613 mL159.3067 mL
5 mM0.6372 mL3.1861 mL6.3723 mL31.8613 mL
10 mM0.3186 mL1.5931 mL3.1861 mL15.9307 mL
20 mM0.1593 mL0.7965 mL1.5931 mL7.9653 mL
50 mM0.0637 mL0.3186 mL0.6372 mL3.1861 mL

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