1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. TRP Channel
  3. HC-067047

HC-067047 is a potent and selective TRPV4 antagonist and reversibly inhibits currents through the human, rat, and mouse TRPV4 orthologs with IC50 values of 48 nM, 133 nM, and 17 nM, respectively.

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

CAS No. : 883031-03-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 41 publication(s) in Google Scholar

Other Forms of HC-067047:

Top Publications Citing Use of Products

41 Publications Citing Use of MCE HC-067047

Others
Cell Imaging/Staining
Bio/Physico-chemical Assay
WB
In Vivo Efficacy Study

    HC-067047 purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2025 Nov 28;10(1):388.  [Abstract]

    HC067047 (100 nM, transient administration) blocked both GSK1016790A (80 nM,transient administration) -evoked inward and outward transmembrane currents in HUVEC cells.

    HC-067047 purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2025 Nov 28;10(1):388.  [Abstract]

    HC067047 (1 µM, 2 h) decreased cell height and increased cell body area in HUVEC cells.

    HC-067047 purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2025 Nov 28;10(1):388.  [Abstract]

    HC067047 (1 µM, 2 h) compromised mitochondrial function, including a reduction in membrane potential, in HUVEC cells.

    HC-067047 purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2025 Nov 28;10(1):388.  [Abstract]

    HC067047 (1 µM, 2 h) increased basal respiration, maximal respiration, ATP production, and spare capacity in HUVEC cells.

    HC-067047 purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2025 Nov 28;10(1):388.  [Abstract]

    HC067047 (1 µM, 2 h) decreased TRPV4, NLRP3, ASC, and p20 caspase-1 protein expression in HUVECs.

    HC-067047 purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2025 Nov 28;10(1):388.  [Abstract]

    HC067047 (10 mg/kg, tail vein injection, every 48 h for 3 weeks) decreased lesion size in the aorta of ApoE-/- mice.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    HC-067047 is a potent and selective TRPV4 antagonist and reversibly inhibits currents through the human, rat, and mouse TRPV4 orthologs with IC50 values of 48 nM, 133 nM, and 17 nM, respectively[1].

    IC50 & Target

    TRPV4

     

    Cellular Effect
    Cell Line Type Value Description References
    CHO-K1 IC50
    57 nM
    Compound: 4; HC067047
    Antagonist activity at human recombinant TRPV4 expressed in CHO-K1 cells assessed as blockade of 1000 nM 4alphaPDD-induced calcium mobilization by FLIPR assay
    Antagonist activity at human recombinant TRPV4 expressed in CHO-K1 cells assessed as blockade of 1000 nM 4alphaPDD-induced calcium mobilization by FLIPR assay
    [PMID: 27637151]
    HEK293 IC50
    48 nM
    Compound: HC-067047
    Antagonist activity at human TRPV4 expressed in HEK293 cells assessed as inhibition of 4alpha-PDD-induced current at holding potential of -40 mV by Whole cell patch-clamp method
    Antagonist activity at human TRPV4 expressed in HEK293 cells assessed as inhibition of 4alpha-PDD-induced current at holding potential of -40 mV by Whole cell patch-clamp method
    [PMID: 28523109]
    In Vitro

    HC-067047 (1 μM; 24 hours; HEI-OC1 cells) treatment significantly decreases mRNA expression in high glucose cultured HEI-OC1 cells[2].
    HC-067047 (1 μM; 24 hours; HEI-OC1 cells) treatment significantly decreases the expression of TRPV4 protein[2].
    HC-067047 (1 μM; 48 hours; HEI-OC1 cells) treatment inhibits cell proliferation[2].
    HC-067047 (1 μM; 48 hours; HEI-OC1 cells) treatment promotes cell apoptosis[2].

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

    RT-PCR[2]

    Cell Line: HEI-OC1 cells
    Concentration: 1 µM
    Incubation Time: 24 hours
    Result: The mRNA expression was significantly decreased.

    Western Blot Analysis[2]

    Cell Line: HEI-OC1 cells
    Concentration: 1 µM
    Incubation Time: 24 hours
    Result: The expression of TRPV4 protein was significantly decreased.

    Cell Proliferation Assay[2]

    Cell Line: HEI-OC1 cells
    Concentration: 1 µM
    Incubation Time: 48 hours
    Result: Inhibited cell proliferation.

    Apoptosis Analysis[2]

    Cell Line: HEI-OC1 cells
    Concentration: 1 µM
    Incubation Time: 48 hours
    Result: Promoted cell apoptosis.
    In Vivo

    HC-067047 (0-50 mg/kg; intraperitoneal injection; for 30 minutes; cyclophosphamide-treated WT and Trpv4 / mice, and naive WT mice) treatment increases functional bladder capacity and reduces micturition frequency in WT mice with cystitis. HC-067047 do not affect bladder function in Trpv4 / mice[1].

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

    Animal Model: Cyclophosphamide-treated WT and Trpv4−/− mice, and naive WT mice[1]
    Dosage: 0 mg/kg, 1 mg/kg, 10 mg/kg, 50 mg/kg
    Administration: Intraperitoneal injection; for 30 minutes
    Result: Increased functional bladder capacity and reduces micturition frequency in WT mice with cystitis and did not affect bladder function in Trpv4−/− mice.
    Molecular Weight

    471.51

    Formula

    C26H28F3N3O2

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1=C(C)N(CCCN2CCOCC2)C(C3=CC=CC=C3)=C1)NC4=CC=CC(C(F)(F)F)=C4

    Shipping

    Room temperature in continental US; may vary elsewhere.

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

    DMSO : 50 mg/mL (106.04 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 2.1208 mL 10.6042 mL 21.2085 mL
    5 mM 0.4242 mL 2.1208 mL 4.2417 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. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • 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 (5.30 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 (5.30 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:  50% PEG300    50% Saline

      Solubility: 25 mg/mL (53.02 mM); Suspended 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).
    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: 99.97%

    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. 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
    DMSO 1 mM 2.1208 mL 10.6042 mL 21.2085 mL 53.0211 mL
    5 mM 0.4242 mL 2.1208 mL 4.2417 mL 10.6042 mL
    10 mM 0.2121 mL 1.0604 mL 2.1208 mL 5.3021 mL
    15 mM 0.1414 mL 0.7069 mL 1.4139 mL 3.5347 mL
    20 mM 0.1060 mL 0.5302 mL 1.0604 mL 2.6511 mL
    25 mM 0.0848 mL 0.4242 mL 0.8483 mL 2.1208 mL
    30 mM 0.0707 mL 0.3535 mL 0.7069 mL 1.7674 mL
    40 mM 0.0530 mL 0.2651 mL 0.5302 mL 1.3255 mL
    50 mM 0.0424 mL 0.2121 mL 0.4242 mL 1.0604 mL
    60 mM 0.0353 mL 0.1767 mL 0.3535 mL 0.8837 mL
    80 mM 0.0265 mL 0.1326 mL 0.2651 mL 0.6628 mL
    100 mM 0.0212 mL 0.1060 mL 0.2121 mL 0.5302 mL
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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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