2. Membrane Transporter/Ion Channel
  3. HCN Channel
  4. Ivabradine hydrochloride

Ivabradine hydrochloride is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine hydrochloride reduces dose-dependently heart rate without modification of blood pressure. Ivabradine hydrochloride shows anticonvulsant, anti-ischaemic and anti-anginal activity.

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Ivabradine hydrochloride Chemical Structure

Ivabradine hydrochloride Chemical Structure

CAS No. : 148849-67-6

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Based on 3 publication(s) in Google Scholar

Other Forms of Ivabradine hydrochloride:

Ivabradine hydrochloride Related Antibodies

Top Publications Citing Use of Products

    Ivabradine hydrochloride purchased from MedChemExpress. Usage Cited in: J Cell Physiol. 2019 Feb;234(2):1925-1936.  [Abstract]

    Protein expression levels of tumor necrosis factor-α (TNF-α), interleukin (IL)-1β, and IL-6 are detected by western blotting.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Ivabradine hydrochloride is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine hydrochloride reduces dose-dependently heart rate without modification of blood pressure. Ivabradine hydrochloride shows anticonvulsant, anti-ischaemic and anti-anginal activity[1][2][3][4].

    In Vivo

    Ivabradine hydrochloride (1, 10, 20 mg/kg; i.p.) shows anticonvulsant and neuroprotective action in mice[3].
    Ivabradine hydrochloride (5, 10, 20 mg/kg;p.o.; daily for 1 weeks) lowers heart rate in mice with enhanced sympathoadrenergic activities[4].

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

    Animal Model: 25-30 g, 6 weeks male Swiss mice[3]
    Dosage: 1, 10, 20 mg/kg
    Administration: I.p.; for 3 days
    Result: Attenuated PTZ- and PICRO-induced seizures while presented an antioxidant effect in all brain areas studied, and reduced cleaved caspase-3 expression in the CA1 and DG region of PICRO- and PTZ-treated mice, respectively.
    Animal Model: 3-4 months transgenic (TG) mice with cardiac-restricted overexpression of b2AR[4]
    Dosage: 5, 10, 20 mg/kg
    Administration: P.o; daily for 1 weeks
    Result: Reduced the maximal HR increase in response to the b-agonist isoproterenol, without modifying the response of contractile parameters at 10 mg/kg.
    Clinical Trial
    Molecular Weight

    505.05

    Formula

    C27H37ClN2O5
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C1N(CCCN(C[C@@H]2C3=CC(OC)=C(OC)C=C3C2)C)CCC4=CC(OC)=C(OC)C=C4C1.Cl
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    H2O : 50 mg/mL (99.00 mM; Need ultrasonic)

    DMSO : 25 mg/mL (49.50 mM; Need ultrasonic; 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 1.9800 mL 9.9000 mL 19.8000 mL
    5 mM 0.3960 mL 1.9800 mL 3.9600 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * 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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    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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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: ≥ 2.5 mg/mL (4.95 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 (4.95 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: 50 mg/mL (99.00 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.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    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).
    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 (sealed storage, away from moisture). 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 / H2O 1 mM 1.9800 mL 9.9000 mL 19.8000 mL 49.5001 mL
    5 mM 0.3960 mL 1.9800 mL 3.9600 mL 9.9000 mL
    10 mM 0.1980 mL 0.9900 mL 1.9800 mL 4.9500 mL
    15 mM 0.1320 mL 0.6600 mL 1.3200 mL 3.3000 mL
    20 mM 0.0990 mL 0.4950 mL 0.9900 mL 2.4750 mL
    25 mM 0.0792 mL 0.3960 mL 0.7920 mL 1.9800 mL
    30 mM 0.0660 mL 0.3300 mL 0.6600 mL 1.6500 mL
    40 mM 0.0495 mL 0.2475 mL 0.4950 mL 1.2375 mL
    H2O 50 mM 0.0396 mL 0.1980 mL 0.3960 mL 0.9900 mL
    60 mM 0.0330 mL 0.1650 mL 0.3300 mL 0.8250 mL
    80 mM 0.0248 mL 0.1238 mL 0.2475 mL 0.6188 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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    Ivabradine hydrochloride 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:

    Ivabradine148849-67-6HCN ChannelHyperpolarization activated cyclic nucleotide gated channelsorally activeheart rateanticonvulsantanti-ischaemicanti-anginalInhibitorinhibitorinhibit

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