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

HC-067047 

Cat. No.: HY-100208 Purity: 99.95%
Handling Instructions

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

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 79 In-stock
Estimated Time of Arrival: December 31
5 mg USD 72 In-stock
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10 mg USD 120 In-stock
Estimated Time of Arrival: December 31
25 mg USD 264 In-stock
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50 mg USD 480 In-stock
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100 mg USD 840 In-stock
Estimated Time of Arrival: December 31
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500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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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]

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].

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].

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.

883031-03-6

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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (106.04 mM; Need ultrasonic)

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
10 mM 0.2121 mL 1.0604 mL 2.1208 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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HC-067047
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