2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel
  4. 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.

HC-067047 Chemical Structure

HC-067047 Chemical Structure

CAS No. : 883031-03-6

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10 mM * 1 mL in DMSO
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Customer Review

Based on 24 publication(s) in Google Scholar

Other Forms of HC-067047:

HC-067047 Related Antibodies

Top Publications Citing Use of Products

View All TRP Channel Isoform Specific Products:

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TRPC TRPM TRPV TRPA TRPML

  • Biological Activity

  • Purity & Documentation

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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

IC50: 48 nM (human TRPV4), 133 nM (rat TRPV4), 17 nM (mouse TRPV4)[1]
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.

HC-067047 Related Antibodies

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

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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: 99.89%

SDS (479 KB)

COA (250 KB) HNMR (270 KB) RP-HPLC (243 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
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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HC-067047 Related Classifications

Help & FAQs
  • 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:

HC-067047883031-03-6HC067047HC 067047TRP ChannelTransient receptor potential channelsInhibitorinhibitorinhibit

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