1. GPCR/G Protein Neuronal Signaling Metabolic Enzyme/Protease
  2. Adrenergic Receptor Endogenous Metabolite
  3. Isoprenaline

Isoprenaline is a non-selective, orally active β-adrenergic receptor agonist. Isoprenaline has potent peripheral vasodilator, bronchodilator, and cardiac stimulating activities. Isoprenaline can be used for the research of bradycardia and bronchial asthma.

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Isoprenaline Chemical Structure

Isoprenaline Chemical Structure

CAS No. : 7683-59-2

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Top Publications Citing Use of Products

54 Publications Citing Use of MCE Isoprenaline

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RT-PCR

    Isoprenaline purchased from MedChemExpress. Usage Cited in: Cell Mol Immunol. 2023 Jan 5.  [Abstract]

    Isoprenaline hydrochloride (ISO; 10 μM; 6 h), markedly inhibits SeV- or HSV-1-induced transcription of the IFNB1 and CXCL10 genes in THP1 cells.

    Isoprenaline purchased from MedChemExpress. Usage Cited in: Cell Mol Immunol. 2023 Jan 5.  [Abstract]

    Isoprenaline hydrochloride (ISO; 10 μM; 0, 3, 6, 9 h) inhibits the phosphorylation of MITAS366, IRF3S386 and STAT1Y701 induced by HSV-1, HSV-2 and HCMV, as well as the phosphorylation of IRF3S386 and STAT1Y701 induced by SeV, EMCV and VSV, in THP1 cells.

    Isoprenaline purchased from MedChemExpress. Usage Cited in: Food Chem Toxicol. 2023 Feb 17;113670.  [Abstract]

    Isoprenaline hydrochloride (ISO; 10 μM; 6 h) pretreatment markedly restores the ATGL and HSL expressions decreased by 1,3-dichloro-2-propanol (1,3-DCP; 100 μM; 6 h) in HepG2 cells.

    Isoprenaline purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2019 Apr 25;38(1):174.   [Abstract]

    EHD1 stabilizes β2AR. A549 cells are incubated in serum-free 1640 medium for 16 h and then treated with ISO (10 μM) for the indicated times in the presence of cycloheximide (CHX, 20 μg/mL). The cell lysates are analyzed by Western blot.

    Isoprenaline purchased from MedChemExpress. Usage Cited in: Naunyn Schmiedebergs Arch Pharmacol. 2018 Dec;391(12):1373-1385.  [Abstract]

    NRCMs are pre-incubated with PCA (50, 100, and 200 μM) for 1 h followed by 10 μM Isoproterenol (ISO) treatment. Cell surface area is measured by rhodamine-phalloidin staining. The expression of β-MHC is detected by Western blot.

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    • Biological Activity

    • Purity & Documentation

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    • Customer Review

    Description

    Isoprenaline is a non-selective, orally active β-adrenergic receptor agonist. Isoprenaline has potent peripheral vasodilator, bronchodilator, and cardiac stimulating activities. Isoprenaline can be used for the research of bradycardia and bronchial asthma[1][2][3][4][5][6].

    Cellular Effect
    Cell Line Type Value Description References
    CHO EC50
    0.003 μM
    Compound: ISO
    Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
    Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
    [PMID: 19581100]
    CHO EC50
    0.003 μM
    Compound: ISO
    Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
    Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
    [PMID: 19232786]
    CHO EC50
    0.012 μM
    Compound: ISO
    Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
    Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
    [PMID: 19581100]
    CHO EC50
    0.012 μM
    Compound: ISO
    Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
    Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
    [PMID: 19232786]
    CHO EC50
    0.084 nM
    Compound: ISP
    Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
    Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
    [PMID: 18307290]
    CHO EC50
    0.084 nM
    Compound: ISP
    Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
    Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
    [PMID: 18553954]
    CHO EC50
    0.084 nM
    Compound: Isoproterenol
    Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
    Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
    [PMID: 15603933]
    CHO EC50
    0.1 μM
    Compound: ISO
    Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
    Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
    [PMID: 19581100]
    CHO EC50
    0.1 μM
    Compound: ISO
    Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
    Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
    [PMID: 19232786]
    CHO EC50
    0.84 nM
    Compound: ISP
    Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
    Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
    [PMID: 19608416]
    CHO EC50
    0.84 nM
    Compound: ISP
    Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
    Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
    [PMID: 19366244]
    CHO EC50
    0.97 nM
    Compound: ISP
    Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
    Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
    [PMID: 18307290]
    CHO EC50
    0.97 nM
    Compound: ISP
    Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
    Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
    [PMID: 19366244]
    CHO EC50
    0.97 nM
    Compound: ISP
    Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
    Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
    [PMID: 18553954]
    CHO EC50
    0.97 nM
    Compound: Isoproterenol
    Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptor
    Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptor
    [PMID: 15603933]
    CHO EC50
    1 μM
    Compound: ISO
    Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
    Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
    [PMID: 19581100]
    CHO EC50
    1 μM
    Compound: ISO
    Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
    Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
    [PMID: 19581100]
    CHO EC50
    1 μM
    Compound: ISO
    Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
    Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
    [PMID: 19581100]
    CHO EC50
    2 nM
    Compound: ISP
    Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
    Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
    [PMID: 19608416]
    CHO EC50
    2 nM
    Compound: ISP
    Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
    Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
    [PMID: 19366244]
    CHO EC50
    2 nM
    Compound: ISP
    Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
    Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
    [PMID: 18553954]
    CHO EC50
    2 nM
    Compound: Isoproterenol
    Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-2 adrenergic receptor
    Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-2 adrenergic receptor
    [PMID: 15603933]
    CHO EC50
    3.9 nM
    Compound: isoproterenol
    Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assay
    Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assay
    [PMID: 18083578]
    CHO EC50
    5.8 nM
    Compound: isoproterenol
    Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
    Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
    [PMID: 18083578]
    CHO EC50
    86 nM
    Compound: isoproterenol
    Agonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 mins
    Agonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 mins
    [PMID: 26125514]
    HEK293 EC50
    120 nM
    Compound: Isoprenaline
    Agonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assay
    Agonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assay
    [PMID: 27132867]
    HEK293 EC50
    87 nM
    Compound: Isoprenaline
    Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
    Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
    [PMID: 27132867]
    In Vitro

    Isoprenaline (300 nM, 3 min) increases particulate cGMP- and cilostamide-inhibited, low-Km cAMP phosphodiesterase (cAMP-PDE) activity by about 100% in intact rat fat cells[1].
    Isoprenaline inhibits insulin-stimulated glucose transport activity in rat adipocytes. Isoprenaline, in the absence of adenosine, promotes a time-dependent (t1/2 approximately 2 min) decrease in the accessibility of insulin-stimulated cell surface GLUT4 of > 50%, which directly correlated with the observed inhibition of transport activity[2].
    Isoprenaline (5 nM and 10 μM) increases cyclic AMP levels and this effect is potentiated by cilostamide (10 mM), by rolipram, a cyclic AMP-specific PDE (PDE 4) inhibitor (10 mM) and by cyclic GMP-elevating agents (50 nM ANF or 30 nM SNP plus 100 nM DMPPO)[3].
    Isoprenaline increases the transcriptional activity of Gi alpha-2 gene to 140% of the control value, whereas gene specific hybridization for Gs alpha remains unchanged[4].
    Isoprenaline (20 nM) increases the amplitude of total iK and causes a negative shift of approximately 10 mV in the activation curve for iK, both in the absence and in the presence of 300 nM nisoldipine to block the L-type Ca2+ current[5].
    Isoprenaline (20 nM) increases the spontaneous pacemaker rate of sino-atrial node pacemaker cells by 16% in rabbit isolated pacemaker cells[5].

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

    In Vivo

    Isoprenaline (oral, 0.27-0. 64 μg/kg) is extensively metabolizes by a relatively small number of reactions in dogs[6].

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

    Animal Model: Dogs[1]
    Dosage: 0.27-0. 64 μg/kg
    Administration: oral
    Result: Excreted largely unchanged in urine, only one-third of the radioactivity in urine was in the form of the O-methyl metabolite.
    Showed plasma radioactivity was almost entirely as conjugated isoprenaline and this metabolite accounted for more than 80% of radioactivity in urine.
    . Showed heart rate returned to base-line values when high plasma concentrations.
    Clinical Trial
    Molecular Weight

    211.26

    Formula

    C11H17NO3

    CAS No.
    SMILES

    OC1=CC=C(C(O)CNC(C)C)C=C1O

    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    Purity & Documentation
    References
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    Product Name:
    Isoprenaline
    Cat. No.:
    HY-108353
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