Zenidolol (ICI-118551) Hydrochloride

Catalog No.S8114 Batch:S811404

Technical Data

Formula	C₁₇H₂₇NO₂.HCl
Molecular Weight	313.86	CAS No.	72795-01-8
Solubility (25°C)*	In vitro	DMSO	63 mg/mL (200.72 mM)
		Ethanol	15 mg/mL (47.79 mM)
		Water	6.25 mg/mL (19.91 mM)
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

Zenidolol (ICI-118551) 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.

Targets

β2-adrenergic receptor ^[1] (Cell-free assay)	β1-adrenergic receptor ^[1] (Cell-free assay)	β3-adrenoceptor ^[1] (Cell-free assay)
0.7nM(Ki)	49.5nM(Ki)	611nM(Ki)

In vitro

ICI-118551 inhibits cAMP accumulation by 50% (IC50 = 1.7 mM)^[1]. 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. ICI 118,551 and 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].

Protocol (from reference)

Cell Assay:^{^[6]}	Cell lines MEF cell line Concentrations 10μM Incubation Time 2-hours incubation at room-temperature Method 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.
Animal Study:^{^[3]}	Animal Models 8-9 weeks old male mice Dosages 1 or 2 mg/kg Administration i.p.

Cell Assay:^{^[6]}

Cell lines
MEF cell line
Concentrations
10μM
Incubation Time
2-hours incubation at room-temperature
Method
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.

Animal Study:^{^[3]}

Animal Models
8-9 weeks old male mice
Dosages
1 or 2 mg/kg
Administration
i.p.

References

+ Expand

Selleck's Zenidolol (ICI-118551) Hydrochloride has been cited by 7 publications

Testicular Macrophages Produce Progesterone De Novo Promoted by cAMP and Inhibited by M1 Polarization Inducers [ Biomedicines, 2022, 10(2)487]	PubMed: 35203696
Functional solubilization of the β2-adrenoceptor using diisobutylene maleic acid [ iScience, 2021, 24(12):103362]	PubMed: 34825145
Development of 3D-QSAR models for predicting the activities of chemicals to stimulate muscle growth via β2-adrenoceptor [ Toxicol In Vitro, 2021, 77:105251]	PubMed: 34601065
Reactivation of dormant tumor cells by modified lipids derived from stress-activated neutrophils [ Sci Transl Med, 2020, 12(572)eabb5817]	PubMed: 33268511
Acute Stress Induces Visceral Hypersensitivity via Glucocorticoid Receptor-Mediated Membrane Insertion of TRPM8: Involvement of a Non-Receptor Tyrosine Kinase Pyk2 [ Neurogastroenterol Motil, 2020, 11;e13877]	PubMed: 32391653
Local Sympathetic Innervations Modulate the Lung Innate Immune Responses [ Sci Adv, 2020, 13;6(20):eaay1497]	PubMed: 32426489
Depression promotes prostate cancer invasion and metastasis via a sympathetic-cAMP-FAK signaling pathway. [ Oncogene, 2018, 37(22):2953-2966]	PubMed: 29515233

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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