1. GPCR/G Protein Neuronal Signaling
  2. Adrenergic Receptor
  3. Zenidolol hydrochloride

Zenidolol hydrochloride  (Synonyms: ICI-118551 hydrochloride)

Cat. No.: HY-13951 Purity: 99.76%
COA Handling Instructions

Zenidolol (ICI-118551) hydrochloride is a highly selective β2 adrenergic receptor antagonist, with Kis of 0.7, 49.5 and 611 nM for β2, β1 and β3 receptors, respectively.

For research use only. We do not sell to patients.

Zenidolol hydrochloride Chemical Structure

Zenidolol hydrochloride Chemical Structure

CAS No. : 72795-01-8

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 106 In-stock
Solution
10 mM * 1 mL in DMSO USD 106 In-stock
Solid
5 mg USD 61 In-stock
10 mg USD 96 In-stock
50 mg USD 300 In-stock
100 mg USD 540 In-stock
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Customer Review

Based on 33 publication(s) in Google Scholar

Other Forms of Zenidolol hydrochloride:

Top Publications Citing Use of Products

    Zenidolol hydrochloride purchased from MedChemExpress. Usage Cited in: Int J Biol Sci. 2023 Apr 2,19.

    Zenidolol (ICI; 10 μM; 2 h) abolishes the Epinephrine-induced phosphorylation of CREB1 in MC38 and HT-29 cells.

    Zenidolol hydrochloride purchased from MedChemExpress. Usage Cited in: J Nutr Biochem. 2018 May 1;58:110-118.  [Abstract]

    PASMCs are pretreated with or not Norepinephrine (50 μM) or ICI 118,551 (5 nM), and α-SMA (D) are analyzed.

    Zenidolol hydrochloride purchased from MedChemExpress. Usage Cited in: Oncol Rep. 2016 Sep;36(3):1576-84.  [Abstract]

    Western blotting of Bcl-2 expression in 8505C lysates after in vitro pharmacologic interventions using propranolol and ICI118551 for 24 h. Western blotting of AKT, p-AKT, mTOR, p-mTOR in 8505C lysates after in vitro pharmacologic interventions using propranolol and ICI118551for 24 h.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Zenidolol (ICI-118551) hydrochloride is a highly selective β2 adrenergic receptor antagonist, with Kis of 0.7, 49.5 and 611 nM for β2, β1 and β3 receptors, respectively.

    IC50 & Target

    β adrenergic receptor

     

    In Vitro

    Zenidolol (ICI-118551) hydrochloride inhibits cAMP accumulation with IC50 of 1.7 μM in IMCD cells[1].
    Zenidolol (ICI-118551; 10 μM) hydrochloride induces a prominent vasorelaxation of norepinephrine (NE)-precontracted PA but not AO[2].
    In failing human heart, Zenidolol (ICI-118551) hydrochloride 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 Zenidolol (ICI-118551) hydrochloride Is Not cAMP-Related. Overexpression of β2AR in rabbit myocytes enhances negative inotropic effects of Zenidolol (ICI-118551) hydrochloride[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    Zenidolol (ICI-118551; 0.2 mg/kg) hydrochloride injected into the jugular vein of the mice, reduces systolic pressure in the pulmonary circuit but not systemic arterial pressure[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Molecular Weight

    313.86

    Formula

    C17H28ClNO2

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CC1=C(CCC2)C2=C(OC[C@H](O)[C@@H](C)NC(C)C)C=C1.[H]Cl

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 33.33 mg/mL (106.19 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 8.33 mg/mL (26.54 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.1861 mL 15.9307 mL 31.8613 mL
    5 mM 0.6372 mL 3.1861 mL 6.3723 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (7.97 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (7.97 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  PBS

      Solubility: 2 mg/mL (6.37 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.76%

    References
    Kinase Assay
    [1]

    One hour prior to assay, the growth media are removed from the wells and replaced with 50 uL of Hanks’balanced salt solution that also contained 0.5 mM of MgCl2•6H2O, 0.4 mM of MgSO4•7H2O, 20 mM of N-2-hydroxyethylpiperazine-N’-2ethanesulfonic acid (HEPES), 1.2 mM of 3-isobutyl-1-methylxanthine (IBMX), 0.95 mM of CaCl2, and 0.05% of BSA. Each plate is placed in a 37°C shaking water bath for dose-response studies. In one study, various doses of isoproterenol (10-9-10-5 M) and β1- and β2-receptor-selective partial agonists (tazolol, prenalterol, salbutamol, and terbutaline, 10-6 and 10-5 M, respectively) are added (5 wells/dose/plate) and incubated for 10 min. In another study, the cells are stimulated with 10 μM isoproterenol in the presence or absence of various doses of β-adrenoceptor antagonists. The incubations are terminated after 10 min by the addition of 100 μL of 10% trichloroacetic acid (TCA) (final TCA concentration of 5%). TCA is removed twice by extraction with H20-saturated ether, and samples are dried at 80°C overnight, prior to resuspension in 50 mM of sodium acetate buffer. The CAMP content is measured with a radioimmunoassay kit.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 3.1861 mL 15.9307 mL 31.8613 mL 79.6534 mL
    5 mM 0.6372 mL 3.1861 mL 6.3723 mL 15.9307 mL
    10 mM 0.3186 mL 1.5931 mL 3.1861 mL 7.9653 mL
    15 mM 0.2124 mL 1.0620 mL 2.1241 mL 5.3102 mL
    20 mM 0.1593 mL 0.7965 mL 1.5931 mL 3.9827 mL
    25 mM 0.1274 mL 0.6372 mL 1.2745 mL 3.1861 mL
    DMSO 30 mM 0.1062 mL 0.5310 mL 1.0620 mL 2.6551 mL
    40 mM 0.0797 mL 0.3983 mL 0.7965 mL 1.9913 mL
    50 mM 0.0637 mL 0.3186 mL 0.6372 mL 1.5931 mL
    60 mM 0.0531 mL 0.2655 mL 0.5310 mL 1.3276 mL
    80 mM 0.0398 mL 0.1991 mL 0.3983 mL 0.9957 mL
    100 mM 0.0319 mL 0.1593 mL 0.3186 mL 0.7965 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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