Name: Zenidolol (ICI-118551) Hydrochloride
Brand: Selleck Chemicals
SKU: S8114
Availability: InStock
Rating: 5 (9 reviews)

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Quality Control

Batch: Purity: 99.45%

99.45

Related Targets	CXCR Hedgehog/Smoothened PKA AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras KRas GPR
Other Adrenergic Receptor Inhibitors	Yohimbine HCl L755507 Atipamezole Higenamine hydrochloride Fenoterol hydrobromide Medetomidine HCl Rauwolscine hydrochloride Deoxycorticosterone acetate Detomidine HCl Naftopidil

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
CHO	Function assay	120 mins	Displacement of [3H]CGP 12177 from human recombinant beta2 adrenergic receptor expressed in CHO cells measured after 120 mins by scintillation counting method, IC50=0.00074μM	27876250
CHOK1	Function assay	2 hrs	Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method, Kd=0.0002455μM	28523097
CHOK1	Function assay	2 hrs	Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method, Kd=0.18197μM	28523097
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 62 mg/mL (197.54 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 62 mg/mL

Water : 21 mg/mL

DMSO : 63 mg/mL (200.72 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 15 mg/mL

Water : 6.25 mg/mL (超声加热十分钟，60℃)

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	313.86	Formula	C₁₇H₂₇NO₂.HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	72795-01-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	ICI-118,551			Smiles	CC1=C2CCCC2=C(C=C1)OCC(C(C)NC(C)C)O.Cl

Mechanism of Action

Targets/IC₅₀/Ki	β2-adrenergic receptor (Cell-free assay) 0.7nM(Ki) β1-adrenergic receptor (Cell-free assay) 49.5nM(Ki) β3-adrenoceptor (Cell-free assay) 611nM(Ki)
In vitro	ICI-118551 inhibits cAMP accumulation by 50% (IC50 = 1.7 mM). 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. 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.
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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/14730417/ [2] https://pubmed.ncbi.nlm.nih.gov/2894217/ [3] https://pubmed.ncbi.nlm.nih.gov/22593095/ [4] https://pubmed.ncbi.nlm.nih.gov/2908820/ [5] https://pubmed.ncbi.nlm.nih.gov/12034656/ [6] https://pubmed.ncbi.nlm.nih.gov/24340001/

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Zenidolol (ICI-118551) Hydrochloride Adrenergic Receptor antagonist

Chemical Structure

Molecular Weight: 313.86