1. GPCR/G Protein
    Neuronal Signaling
  2. Adrenergic Receptor
  3. ICI 118,551 hydrochloride

ICI 118,551 hydrochloride (Synonyms: ICI 118551 hydrochloride)

Cat. No.: HY-13951 Purity: 98.50%
Handling Instructions

ICI 118,551 (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.

ICI 118,551 hydrochloride Chemical Structure

ICI 118,551 hydrochloride Chemical Structure

CAS No. : 72795-01-8

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10 mM * 1 mL in DMSO USD 106 In-stock
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Customer Review

Based on 7 publication(s) in Google Scholar

Top Publications Citing Use of Products

    ICI 118,551 hydrochloride purchased from MCE. Usage Cited in: Oncol Rep. 2016 Sep;36(3):1576-84.

    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.

    ICI 118,551 hydrochloride purchased from MCE. Usage Cited in: J Nutr Biochem. 2018 May 1;58:110-118.

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

    • Protocol

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    • References

    • Customer Review

    Description

    ICI 118,551 (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

    Ki: 0.7nM (β2 receptor), 49.5 nM (β1 receptor), 611 nM (β3 receptor)[4]

    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].

    Molecular Weight

    313.86

    Formula

    C₁₇H₂₈ClNO₂

    CAS No.

    72795-01-8

    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 25 mg/mL (79.65 mM; Need ultrasonic)

    H2O : 12.5 mg/mL (39.83 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
    10 mM 0.3186 mL 1.5931 mL 3.1861 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

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

    *All of the co-solvents are provided by MCE.
    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
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    Product Name:
    ICI 118,551 hydrochloride
    Cat. No.:
    HY-13951
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