Cat. No.: HY-100208

HC-067047

Name: HC-067047
Brand: MedChemExpress
SKU: HY-100208
Price: 79.00 USD
Availability: InStock
Rating: 5 (45 reviews)

45 Cited Publications

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Based on 45 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.

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Pureté : 99.97%
CAS No.: 883031-03-6
Formule: C₂₆H₂₈F₃N₃O₂
Masse moléculaire:471.51

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

HC-067047 Chemical Structure

CAS No.: 883031-03-6

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (45)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

TRPV4

Voir tous les produits spécifiques à Isoform TRP Channel :

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]

View Protocol

Cell Line:

HEI-OC1 cells
Concentration:

1 µM
Incubation Time:

24 hours
Result:

The mRNA expression was significantly decreased.

Western Blot Analysis^[2]

View Protocol

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]

View Protocol

Cell Line:

HEI-OC1 cells
Concentration:

1 µM
Incubation Time:

48 hours
Result:

Inhibited cell proliferation.

Apoptosis Analysis^[2]

View Protocol

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.

Chemical Information

CAS No. 883031-03-6
Appearance Solid
Masse moléculaire 471.51
Formule 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
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (45)

All OthersCell Imaging/StainingBio/Physico-chemical AssayWBIn Vivo Efficacy Study

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Journal Impact Factor

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

Gear-like MOF microrobots for single cell mechanotransduction of microvilli. [Abstract]

2026 Feb 26;17(1):3254. PMID: 41748583
ACS Nano

2026 Jul 28;20(29):20730-20746. PMID: 42453052
Redox Biol

TRPV4 drives macrophage pyroptosis via mitochondrial dysfunction and mtROS-dependent NLRP3 inflammasome activation in acute lung injury. [Abstract]

2026 Jun 11:95:104255. PMID: 42314332
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
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
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
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
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
Life Sci

Identification and regulation of a novel leptin receptor-linked enhancer during zebrafish ventricle regeneration. [Abstract]

2025 Feb 15:363:123415. PMID: 39864617
Transl Res

TRPV4 in adipose tissue ameliorates diet-induced obesity by promoting white adipocyte browning. [Abstract]

2024 Apr:266:16-31. PMID: 37926276
Eur J Pharmacol

Morin ameliorates coronary artery relaxation by activating TRPV4-eNOS-NO signalling in high-salt diet-fed rats. [Abstract]

2025 Sep 5:1002:177807. PMID: 40472987
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

Pregabalin inhibits purinergic P2Y2 receptor and TRPV4 to suppress astrocyte activation and to relieve neuropathic pain. [Abstract]

2023 Dec 5:960:176140. PMID: 37925132
Acta Physiol

The CaSR/TRPV4 coupling mediates pro-inflammatory macrophage function. [Abstract]

2023 Apr;237(4):e13926. PMID: 36606511
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
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
Front Pharmacol

Role of Serosal TRPV4-Constituted SOCE Mechanism in Secretagogues-Stimulated Intestinal Epithelial Anion Secretion. [Abstract]

2021 Jul 14:12:684538. PMID: 34335254
ACS Omega

Identification of Phialomustin‑B (PHL-B) as a Novel Natural TRPA1 Channel Inhibitor. [Abstract]

2025 Aug 21;10(34):39192-39202. PMID: 40918390
Brain Pathol

Targeting TRPV4 to restore glymphatic system function and alleviate cerebral edema in ischemic stroke. [Abstract]

2025 Nov;35(6):e70022. PMID: 40481713
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
Cell Signal

TRPV4 blockade alleviates endoplasmic reticulum stress mediated apoptosis in hypoxia-induced cardiomyocyte injury. [Abstract]

2024 Feb:114:110973. PMID: 37981067
iScience

2026 Aug 27;29(9):117304. PMID: 42707181
Aquaculture

2021, 736537.
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
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
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
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
Exp Eye Res

TRPV4 channels promote vascular permeability in retinal vascular disease. [Abstract]

2023 Mar:228:109405. PMID: 36773739
Neurogastroenterol Motil

Shugan Decoction Ameliorated WAS-Induced Abnormal Colonic Motility in Rats by Inhibiting Colonic TRPV4-PGE2 Signaling. [Abstract]

2025 Dec;37(12):e70104. PMID: 40545667
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
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
Traditional Medicine Research

2026;11(2):11.
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
Dublin City University

2026.
SSRN

2025 Dec 12.
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
Research Square Preprint

2021 Dec.
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

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1208 mL

10.6042 mL

21.2085 mL

5 mM

0.4242 mL

2.1208 mL

4.2417 mL

10 mM

0.2121 mL

1.0604 mL

2.1208 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.30 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during 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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (280 KB)
SDS (480 KB)
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- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

45 Cited Publications

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HC-067047

Publications Citing Use of MedChemExpress (MCE) HC-067047

Voir tous les produits spécifiques à Isoform TRP Channel