HC-067047
Based on 41 publication(s) in Google Scholar
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.
- Purity: 99.97%
- CAS No.: 883031-03-6
- Formula: C26H28F3N3O2
- Molecular Weight:471.51
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
Membrane Transporter/Ion Channel Compound Library
HY-L011
-
Neuronal Signaling Compound Library
HY-L013
-
Anti-Cancer Compound Library
HY-L025
-
Mechanoreceptors Compound Library
HY-L095
-
Pain-Related Compound Library
HY-L139
-
Membrane Protein-targeted Compound Library
HY-L149
-
Membrane Receptor-targeted Compound Library
HY-L150
-
Highly Selective Inhibitors Library
HY-L158
-
Ion Channel Compound Library
HY-L166
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
Publications Citing Use of MedChemExpress (MCE) HC-067047
More- Signal Transduct Target Ther. 2025 Nov 28;10(1):388. [Abstract]
- Nat Immunol. 2026 May;27(5):949-960. [Abstract]
- Nat Commun. 2026 Feb 26;17(1):3254. [Abstract]
- Cell Death Dis. 2023 Jun 28;14(6):379. [Abstract]
- Acta Pharmacol Sin. 2023 Apr;44(4):811-821. [Abstract]
- Biomed Pharmacother. 2020 Feb;122:109697. [Abstract]
- Biomed Pharmacother. 2018 Dec:108:540-546. [Abstract]
- Environ Pollut. 2020 Jan;256:113375. [Abstract]
- Sci Signal. 2025 Dec 23;18(918):eadt1539. [Abstract]
- Antioxidants (Basel). 2022 Nov 23;11(12):2315. [Abstract]
- Brain Pathol. 2025 Jun 7:e70022. [Abstract]
- Transl Res. 2024 Apr:266:16-31. [Abstract]
- Acta Neuropathol Commun. 2025 Apr 10;13(1):73. [Abstract]
- Acta Physiol. 2023 Apr;237(4):e13926. [Abstract]
- Life Sci. 2025 Jan 24:123415. [Abstract]
- Cell Mol Neurobiol. 2023 Apr;43(3):1283-1300. [Abstract]
- Front Pharmacol. 2021 Jul 14:12:684538. [Abstract]
- Int Immunopharmacol. 2025 Sep 10:165:115453. [Abstract]
- Eur J Pharmacol. 2025 Sep 15:1003:177900. [Abstract]
- Eur J Pharmacol. 2025 Jun 3:177807. [Abstract]
- Eur J Pharmacol. 2023 Dec 5:960:176140. [Abstract]
- ACS Omega. 2025 Aug 21;10(34):39192-39202. [Abstract]
- Mol Neurobiol. 2025 Mar;62(3):3615-3629. [Abstract]
- J Cell Physiol. 2023 Nov;238(11):2692-2709. [Abstract]
- Sci Rep. 2025 Nov 24;15(1):41644. [Abstract]
- J Biol Chem. 2022 May;298(5):101847. [Abstract]
- Aquaculture. 2021, 736537.
- Cell Signal. 2024 Feb:114:110973. [Abstract]
- Heliyon. 2023 Jun 23;9(7):e17583. [Abstract]
- Am J Physiol Lung Cell Mol Physiol. 2020 Apr 1;318(4):L723-L741. [Abstract]
- J Cancer. 2025 Jan 13;16(4):1324-1334. [Abstract]
- Neurogastroenterol Motil. 2025 Jun 22:e70104. [Abstract]
- Mol Pain. 2024 Jan-Dec:20:17448069241272149. [Abstract]
- Exp Eye Res. 2023 Mar:228:109405. [Abstract]
- Physiol Behav. 2026 Feb:304:115159. [Abstract]
- Exp Ther Med. 2022 Jun 1;24(1):478. [Abstract]
- Biomed Res Int. 2022 Jan 4:2022:2777882. [Abstract]
- Biol Bull. 2022 Feb;242(1):48-61. [Abstract]
- SSRN. 2025 Dec 12.
- Traditional Medicine Research. 2026;11(2):11.
- Research Square Preprint. 2021 Dec.
Customer Validation & Images
-
Others
-
Cell Imaging/Staining
-
Cell Imaging/Staining
-
Bio/Physico-chemical Assay
-
WB
Biological Activity
|
TRPV4 |
|
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] |
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.
-
Cell Line:HEI-OC1 cells
-
Concentration:1 µM
-
Incubation Time:24 hours
-
Result:The mRNA expression was significantly decreased.
-
Cell Line:HEI-OC1 cells
-
Concentration:1 µM
-
Incubation Time:24 hours
-
Result:The expression of TRPV4 protein was significantly decreased.
-
Cell Line:HEI-OC1 cells
-
Concentration:1 µM
-
Incubation Time:48 hours
-
Result:Inhibited cell proliferation.
-
Cell Line:HEI-OC1 cells
-
Concentration:1 µM
-
Incubation Time:48 hours
-
Result:Promoted cell apoptosis.
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.
Chemical Information
-
CAS No. 883031-03-6
-
Appearance Solid
-
Molecular Weight 471.51
-
Formula C26H28F3N3O2
-
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
Publications (41)
-
Journal Impact Factor
-
Most Recent
-
Signal Transduct Target Ther
Pulsed electromagnetic fields inhibit atherosclerosis by regulating pyroptosis through membrane tension-mediated mechanosensitive channels. [Abstract]2025 Nov 28;10(1):388. PMID: 41309549
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.
-
Nat Immunol
Lipid asymmetry disruption by XKR8 orchestrates neutrophil extracellular trap formation and inhibits fungal infection. [Abstract]2026 May;27(5):949-960. PMID: 41781710 -
Nat Commun
2026 Feb 26;17(1):3254. PMID: 41748583 -
Cell Death Dis
Inhibition of TRPV4 remodels single cell polarity and suppresses the metastasis of hepatocellular carcinoma. [Abstract]2023 Jun 28;14(6):379. PMID: 37369706 -
Acta Pharmacol Sin
TRPV4 channel is involved in HSV-2 infection in human vaginal epithelial cells through triggering Ca2+ oscillation. [Abstract]2023 Apr;44(4):811-821. PMID: 36151392 -
Biomed Pharmacother
The effect of transient receptor potential vanilloid 4 on the intestinal epithelial barrier and human colonic cells was affected by tyrosine-phosphorylated claudin-7. [Abstract]2020 Feb;122:109697. PMID: 31918271 -
Biomed Pharmacother
The effect of serine phosphorylated claudin-7 on the epithelial barrier and the modulation by transient receptor potential vanilloid 4 in human colonic cells. [Abstract]2018 Dec:108:540-546. PMID: 30243087 -
Environ Pollut
Exposure to both formaldehyde and high relative humidity exacerbates allergic asthma by activating the TRPV4-p38 MAPK pathway in Balb/c mice. [Abstract]2020 Jan;256:113375. PMID: 31662264 -
Sci Signal
The mechanosensitive channel TRPV4 inhibits pulmonary inflammation by limiting NF-κB signaling in alveolar macrophages. [Abstract]2025 Dec 23;18(918):eadt1539. PMID: 41433421 -
Antioxidants (Basel)
Blocking TRPV4 Ameliorates Osteoarthritis by Inhibiting M1 Macrophage Polarization via the ROS/NLRP3 Signaling Pathway. [Abstract]2022 Nov 23;11(12):2315. PMID: 36552524 -
Brain Pathol
Targeting TRPV4 to restore glymphatic system function and alleviate cerebral edema in ischemic stroke. [Abstract]2025 Jun 7:e70022. PMID: 40481713 -
Transl Res
TRPV4 in adipose tissue ameliorates diet-induced obesity by promoting white adipocyte browning. [Abstract]2024 Apr:266:16-31. PMID: 37926276 -
Acta Neuropathol Commun
Transient receptor potential vanilloid 4 blockage attenuates pyroptosis in hippocampus of mice following pilocarpine‑induced status epilepticus. [Abstract]2025 Apr 10;13(1):73. PMID: 40205503 -
Acta Physiol
2023 Apr;237(4):e13926. PMID: 36606511 -
Life Sci
Identification and regulation of a novel leptin receptor-linked enhancer during zebrafish ventricle regeneration. [Abstract]2025 Jan 24:123415. PMID: 39864617 -
Cell Mol Neurobiol
Blockage of TRPV4 Downregulates the Nuclear Factor-Kappa B Signaling Pathway to Inhibit Inflammatory Responses and Neuronal Death in Mice with Pilocarpine-Induced Status Epilepticus. [Abstract]2023 Apr;43(3):1283-1300. PMID: 35840809 -
Front Pharmacol
Role of Serosal TRPV4-Constituted SOCE Mechanism in Secretagogues-Stimulated Intestinal Epithelial Anion Secretion. [Abstract]2021 Jul 14:12:684538. PMID: 34335254 -
Int Immunopharmacol
Osthole alleviates neuropathic pain by suppressing astrocytes activation and associated inflammatory responses via the PKCδ/TRPV4 signaling pathway. [Abstract]2025 Sep 10:165:115453. PMID: 40934539 -
Eur J Pharmacol
Novel mechanisms of metformin-induced vasorelaxation of mesenteric arterioles via endothelium-dependent hyperpolarization to treat murine colitis. [Abstract]2025 Sep 15:1003:177900. PMID: 40617384 -
Eur J Pharmacol
Morin ameliorates coronary artery relaxation by activating TRPV4-eNOS-NO signalling in high-salt diet-fed rats. [Abstract]2025 Jun 3:177807. PMID: 40472987 -
Eur J Pharmacol
Pregabalin inhibits purinergic P2Y2 receptor and TRPV4 to suppress astrocyte activation and to relieve neuropathic pain. [Abstract]2023 Dec 5:960:176140. PMID: 37925132 -
ACS Omega
2025 Aug 21;10(34):39192-39202. PMID: 40918390 -
Mol Neurobiol
TRPV4 Blockage Inhibits the Neurogenesis in the Adult Hippocampal Dentate Gyrus Following Pilocarpine‑Induced Status Epilepticus. [Abstract]2025 Mar;62(3):3615-3629. PMID: 39312069 -
J Cell Physiol
Simulated microgravity-induced oxidative stress and loss of osteogenic potential of osteoblasts can be prevented by protection of primary cilia. [Abstract]2023 Nov;238(11):2692-2709. PMID: 37796139 -
Sci Rep
The TRPV4-YAP axis mediates cytoskeletal and extracellular matrix remodeling in trabecular meshwork cells as a novel glaucoma mechanism. [Abstract]2025 Nov 24;15(1):41644. PMID: 41286165 -
J Biol Chem
Capsaicin inhibits intestinal Cl- secretion and promotes Na+ absorption by blocking TRPV4 channels in healthy and colitic mice. [Abstract]2022 May;298(5):101847. PMID: 35314195 -
-
Cell Signal
TRPV4 blockade alleviates endoplasmic reticulum stress mediated apoptosis in hypoxia-induced cardiomyocyte injury. [Abstract]2024 Feb:114:110973. PMID: 37981067 -
Heliyon
The role of TRPV4 in the regulation of retinal ganglion cells apoptosis in rat and mouse. [Abstract]2023 Jun 23;9(7):e17583. PMID: 37456002 -
Am J Physiol Lung Cell Mol Physiol
Adipose-derived exosomes protect the pulmonary endothelial barrier in ventilator-induced lung injury by inhibiting the TRPV4/Ca2+ signaling pathway. [Abstract]2020 Apr 1;318(4):L723-L741. PMID: 32073873 -
J Cancer
Matrix stiffness regulates NPC invasiveness by modulating a mechanoresponsive TRPV4-Nox4-IL-8 signaling axis. [Abstract]2025 Jan 13;16(4):1324-1334. PMID: 39895789 -
Neurogastroenterol Motil
Shugan Decoction Ameliorated WAS-Induced Abnormal Colonic Motility in Rats by Inhibiting Colonic TRPV4-PGE2 Signaling. [Abstract]2025 Jun 22:e70104. PMID: 40545667 -
Mol Pain
Histamine H4 receptor and TRPV1 mediate itch induced by cadaverine, a metabolite of the microbiome. [Abstract]2024 Jan-Dec:20:17448069241272149. PMID: 39079948 -
Exp Eye Res
2023 Mar:228:109405. PMID: 36773739 -
Physiol Behav
Rising TRPV4 expression in the central nucleus of amygdala is involved in tooth movement pain. [Abstract]2026 Feb:304:115159. PMID: 41203189 -
Exp Ther Med
Ketamine administration ameliorates anesthesia and surgery-induced cognitive dysfunction via activation of TRPV4 channel opening. [Abstract]2022 Jun 1;24(1):478. PMID: 35761804 -
Biomed Res Int
Role of TRPV4 in the Diagnosis and Treatment of Helicobacter pylori Infection in Children with Duodenal Ulcers. [Abstract]2022 Jan 4:2022:2777882. PMID: 35028313 -
Biol Bull
Functional Characterization of TRPV-Like Ion Channels Involved in Nematocyst Discharge from the Sea Anemone Diadumene lineata. [Abstract]2022 Feb;242(1):48-61. PMID: 35245164 -
-
-
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 25 mg/mL (53.02 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
-
Data Sheet (280 KB)
-
SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Portuguese - PT (480 KB)
-
Handling Instructions (2659 KB)
References
[1]. Everaerts W et al. Inhibition of the cation channel TRPV4 improves bladder function in mice and rats with cyclophosphamide-induced cystitis.Proc Natl Acad Sci U S A. 2010 Nov 2;107(44):19084-9. [Content Brief]
[2]. Xing Y, et al. Decreased Expression of TRPV4 Channels in HEI-OC1 Cells Induced by High Glucose Is Associated with Hearing Impairment. Yonsei Med J. 2018 Nov;59(9):1131-1137. [Content Brief]
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 |
Powered by Bioz