2. GPCR/G Protein Neuronal Signaling Apoptosis Metabolic Enzyme/Protease
  3. Adrenergic Receptor Apoptosis Caspase Bcl-2 Family HIF/HIF Prolyl-Hydroxylase
  4. Zenidolol

Zenidolol (ICI-118551) is a selective β2-adrenergic receptor antagonist with Ki values of Zenidolol for β2, β1 and β3 adrenergic receptors of 0.7, 49.5 and 611 nM, respectively. Zenidolol exerts antitumor effects via inducing apoptosis, inhibiting tumor sphere formation, and downregulating the HIF pathway by blocking β2-AR on tumor cells. Zenidolol exhibits a unique pulmonary vessel-specific vasodilatory effect in mouse models. Zenidolol can be used as an intraocular pressure-lowering agent in ophthalmic disease research.

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

CAS No. : 72795-26-7

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Customer Review

Based on 45 publication(s) in Google Scholar

Other Forms of Zenidolol:

Zenidolol Related Antibodies

Top Publications Citing Use of Products

45 Publications Citing Use of MCE Zenidolol

Cell Proliferation/Viability Assay
IF
WB
Cell Imaging/Staining

    Zenidolol purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Oct 6:e04817.  [Abstract]

    Zenidolol (ICI118551; ICI) (1 µM; 24-72 H) reversed the NE‐induced reduction in Sertoli cell viability.

    Zenidolol purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Oct 6:e04817.  [Abstract]

    Zenidolol (ICI118551; ICI) (1 µM) reversed NE-induced ACSL4 increase and GPX4 decrease in Sertoli cells.

    Zenidolol purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Oct 6:e04817.  [Abstract]

    Zenidolol (ICI118551; ICI) (1 µM) reversed NE-induced alterations in the expression of SLC7A11, GPX4, and ACSL4 in TM4 cells.

    Zenidolol purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Oct 6:e04817.  [Abstract]

    Zenidolol (ICI118551; ICI) (1 µM) alleviated the NE-induced increase in death of TM4 cells.

    Zenidolol purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Oct 6:e04817.  [Abstract]

    Zenidolol (ICI118551; ICI) (1 µM) normalized tight junction markers ZO-1 and Claudin-11 protein levels in TM4 cells suppressed by NE.

    Zenidolol purchased from MedChemExpress. Usage Cited in: Int J Biol Sci. 2023 Apr 2;19(7):2006-2019.

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

    Zenidolol purchased from MedChemExpress. Usage Cited in: J Nutr Biochem. 2018 Aug: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 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.

    View All Adrenergic Receptor Isoform Specific Products:

    View All Isoforms
    α adrenergic receptor β adrenergic receptor

    View All Caspase Isoform Specific Products:

    View All Isoforms
    Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

    View All Bcl-2 Family Isoform Specific Products:

    View All Isoforms
    Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

    View All HIF/HIF Prolyl-Hydroxylase Isoform Specific Products:

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    HIF-1α HIF

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Zenidolol (ICI-118551) is a selective β2-adrenergic receptor antagonist with Ki values of Zenidolol for β2, β1 and β3 adrenergic receptors of 0.7, 49.5 and 611 nM, respectively. Zenidolol exerts antitumor effects via inducing apoptosis, inhibiting tumor sphere formation, and downregulating the HIF pathway by blocking β2-AR on tumor cells. Zenidolol exhibits a unique pulmonary vessel-specific vasodilatory effect in mouse models. Zenidolol can be used as an intraocular pressure-lowering agent in ophthalmic disease research[1][2][3][4][5].

    In Vitro

    Zenidolol (0-200 μM; 48 h) reduces the cell viability of primary cultured hemangioblastomas derived from VHL in a dose-dependent manner, and exhibits higher specificity for HB cells compared with HUVECs[1].
    Zenidolol (100 μM; 7 days) inhibits glomeruloid body formation in primary cultures of hemangioblastomas derived from VHL tumors[1].
    Zenidolol (100 μM; 6 h) inhibits endothelial cell migration and angiogenesis in human umbilical vein endothelial cells (HUVECs)[1].
    Zenidolol (100 μM; 48 h) attenuates hypoxia-induced nuclear translocation of HIF-1α in human umbilical vein endothelial cells (HUVECs) and primary cultures of VHL-derived hemangioblastomas[1].
    Zenidolol (100 μM; 72 h) induces apoptosis in primary cultures of VHL-derived hemangioblastomas by increasing caspase 3/7/9 activity and upregulating the pro-apoptotic gene BAX[1].
    Zenidolol (100 μM; 48-72 h) inhibits the expression of AQP-1, a HIF target gene, in primary cultures of hemangioblastoma derived from VHL[1].
    Zenidolol (10 μM) induces nitric oxide production in bovine pulmonary artery endothelial cells and promotes phosphorylation of the Ser1177 site of endothelial nitric oxide synthase[4].

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

    Zenidolol Related Antibodies

    Cell Viability Assay[1]

    Cell Line: von Hippel-Lindau (VHL) disease-derived hemangioblastoma (HB) primary cultures, human umbilical vein endothelial cells (HUVECs)
    Concentration: 0, 25, 50, 100 and 200 μM
    Incubation Time: 48 h
    Result: Decreased the viability of HB primary culture cells in a dose-dependent manner, with viability dropping to 40-45% at 100 μM compared to untreated cells. Maintained HUVEC viability at 80% at 100 μM compared to untreated cells.

    Cell Migration Assay[1]

    Cell Line: human umbilical vein endothelial cells (HUVECs)
    Concentration: 100 μM
    Incubation Time: 6 h
    Result: Delayed wound closure in HUVECs, significantly impairing endothelial cell migration compared to untreated controls.

    Immunofluorescence[1]

    Cell Line: hypoxia-induced human umbilical vein endothelial cells (HUVECs), von Hippel-Lindau (VHL) disease-derived hemangioblastoma (HB) primary cultures
    Concentration: 100 μM
    Incubation Time: 48 h
    Result: Shifted HIF-1α localization from predominantly nuclear to a mix of cytoplasmic and nuclear in DFO-treated HUVECs compared to controls.
    Reduced nuclear HIF-1α localization in HB cells compared to untreated controls, where HIF-1α was mainly nuclear.

    Apoptosis Analysis[1]

    Cell Line: von Hippel-Lindau (VHL) disease-derived hemangioblastoma (HB) primary cultures
    Concentration: 100 μM
    Incubation Time: 72 h
    Result: Induced a 1.7-fold increase in caspase 3/7 activity in HB cells compared to untreated controls. Significantly upregulated mRNA expression of BAX (1.3-2 fold) and Caspase 9 (1.3-2 fold) compared to untreated controls.

    Real Time qPCR[1]

    Cell Line: von Hippel-Lindau (VHL) disease-derived hemangioblastoma (HB) primary cultures (HB19, HB23, HB28)
    Concentration: 100 μM
    Incubation Time: 48 and 72 h
    Result: Significantly decreased mRNA expression of AQP-1 (a HIF-1α target gene) in multiple HB primary cultures compared to untreated controls.

    Western Blot Analysis[4]

    Cell Line: bovine pulmonary arterial endothelial cells (bPAECs)
    Concentration: 10 μM
    Incubation Time: 2, 5, 10 minutes
    Result: Induced time-dependent phosphorylation of eNOS at Ser1177, with normalized p-eNOS/β-actin values increasing over the 10-minute incubation period.
    In Vivo

    Zenidolol (5-500 μg/kg; i.v.; cumulative administration) is a potent β2-selective adrenergic receptor antagonist. In anesthetized Beagle dogs, its affinity for vascular β2-receptors is at least 250-fold higher than that for cardiac β1-receptors[2].
    Zenidolol (50-1000 μg/kg; i.v.; cumulative administration) at doses that block vascular β2-adrenoceptors does not affect the cardiac responses to sympathetic nerve stimulation in anesthetized Beagle dogs, whereas the high dose (1 mg/kg) inhibits SNS-induced heart rate elevation[2].
    Zenidolol (0.25-2.0%, 30 μg/kg; topical ocular administration, subcutaneous administration; single dose) is a potent ocular hypotensive agent with extremely low cardiac side effects, and it weakly blocks cardiac β-adrenergic receptor-mediated responses[3].
    Zenidolol (0.2 mg/kg; intravenous injection via jugular vein; single administration) significantly reduces pulmonary arterial systolic pressure in mice, but has no effect on systemic arterial systolic pressure[4].

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

    Animal Model: Beagle dogs (either sex, weight 10-15 kg, anaesthetised with pentobarbitone sodium)[2]
    Dosage: 5, 10, 20, 40, 100, 200, 500 μg/kg
    Administration: i.v.; cumulative; each dose given 10 minutes before isoproterenol dose-response curve construction
    Result: Caused a dose-dependent parallel shift to the right of the isoproterenol vasodilator curve; did not significantly alter isoproterenol chronotropic response curves even at the highest dose of 500 μg/kg (0.5 mg/kg); showed an effective dissociation constant (Kᵦ') of 2.1 μg/kg at vascular β₂-receptors; exhibited at least a 250-fold greater affinity for vascular β₂-receptors than cardiac β₁-receptors.
    Animal Model: Beagle dogs (either sex, weight 10-18 kg, anaesthetised with pentobarbitone sodium)[2]
    Dosage: 50, 200, 1000 μg/kg (1 mg/kg)
    Administration: i.v.; cumulative
    Result: Caused a 10-30-fold shift to the right of the isoproterenol vasodilator dose-response curve at 50, 200 μg/kg without significantly reducing heart rate increases due to sympathetic nerve stimulation (SNS); induced significant antagonism of the SNS chronotropic response at the highest dose of 1000 μg/kg (1 mg/kg).
    Animal Model: Beagle dogs (either sex, weight 10-17 kg, anaesthetised with pentobarbitone sodium)[2]
    Dosage: 10, 20, 40, 100, 200, 1000 μg/kg
    Administration: i.v.; cumulative
    Result: Produced no significant changes in resting heart rate, LV dP/dtₘₐₓ, diastolic blood pressure, or AVCT over the dose range 10-1000 μg/kg; caused a trend toward reduced aortic flow, likely due to prolonged anaesthesia rather than the reagent itself.
    Animal Model: New Zealand white (male, 2-4 kg)[3]
    Dosage: 0.25%, 0.5%, 1.0%, 2.0% (topical ocular IOP studies); 30 μg/kg (subcutaneous IOP studies); 1% (topical ocular cardiac response study)
    Administration: topical ocular, 50 μl or two 25 μl doses 5 min apart; s.c., single dose
    Result: Caused a dose-dependent IOP decrease (maximal 4.2 mmHg at 1% at 1 hour post-administration; significant decreases at 0.25%, 0.5%, 1.0%, 2.0%).
    Showed a greater and more prolonged IOP decrease in time-course studies, with maximal effect at 1-3 hours and persistence beyond 4 hours.
    Induced a rapid IOP decrease (maximal at 1 hour, returning to normal by 6 hours) after subcutaneous 30 μg/kg administration.
    Exhibited an IC50 of 176 μg/kg for blocking isoprenaline-induced cardio-acceleration when given systemically. Produced no effect on cardiac response to isoprenaline when given topically.
    Animal Model: KO mice (C57/Bl6)[4]
    Dosage: 0.2 mg/kg
    Administration: Intravenous injection via jugular vein; single administration
    Result: Significantly reduced pulmonary artery systolic pressure (by approximately 25%), but has no effect on systemic artery systolic pressure.
    Molecular Weight

    277.40

    Formula

    C17H27NO2
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    C[C@@H](NC(C)C)[C@@H](O)COC1=CC=C(C)C2=C1CCC2
    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 : 100 mg/mL (360.49 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.6049 mL 18.0245 mL 36.0490 mL
    5 mM 0.7210 mL 3.6049 mL 7.2098 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    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: ≥ 5 mg/mL (18.02 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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% Corn Oil

      Solubility: ≥ 5 mg/mL (18.02 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    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.
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    Purity & Documentation
    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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.6049 mL 18.0245 mL 36.0490 mL 90.1226 mL
    5 mM 0.7210 mL 3.6049 mL 7.2098 mL 18.0245 mL
    10 mM 0.3605 mL 1.8025 mL 3.6049 mL 9.0123 mL
    15 mM 0.2403 mL 1.2016 mL 2.4033 mL 6.0082 mL
    20 mM 0.1802 mL 0.9012 mL 1.8025 mL 4.5061 mL
    25 mM 0.1442 mL 0.7210 mL 1.4420 mL 3.6049 mL
    30 mM 0.1202 mL 0.6008 mL 1.2016 mL 3.0041 mL
    40 mM 0.0901 mL 0.4506 mL 0.9012 mL 2.2531 mL
    50 mM 0.0721 mL 0.3605 mL 0.7210 mL 1.8025 mL
    60 mM 0.0601 mL 0.3004 mL 0.6008 mL 1.5020 mL
    80 mM 0.0451 mL 0.2253 mL 0.4506 mL 1.1265 mL
    100 mM 0.0360 mL 0.1802 mL 0.3605 mL 0.9012 mL
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    Zenidolol Related Classifications

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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.

    Keywords:

    Zenidolol72795-26-7ICI-118551ICI118551ICI 118551Adrenergic ReceptorApoptosisCaspaseBcl-2 FamilyHIF/HIF Prolyl-HydroxylaseBeta ReceptorHypoxia-inducible factorsHIFsHIF-PHangiogenesisHIF-1αβ1-adrenoceptorsblood-brain barrierHIF signalingapoptosisβ2-adrenergic receptorHeLa 9xHRE-Luc cellsHUVECsβ3-adrenoceptorsInhibitorinhibitorinhibit

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