1. Metabolic Enzyme/Protease NF-κB Neuronal Signaling Membrane Transporter/Ion Channel Immunology/Inflammation
  2. Glutathione S-transferase NF-κB Calcium Channel NO Synthase
  3. Ethacrynic acid

Ethacrynic acid  (Synonyms: Etacrynic acid)

Cat. No.: HY-B1640 Purity: 99.90%
COA Handling Instructions

Ethacrynic acid has anti-inflammatory and anticancer activity. Ethacrynic acid is an orally active diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferase (GSTs) and Wnt signaling pathways. Ethacrynic acid is a radiosensitizer. Ethacrynic acid can inhibit airway smooth muscle (ASM) contraction in mice. Ethacrynic acid can increase the outflow of aqueous humor from the eye for the study of glaucoma.

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

Ethacrynic acid Chemical Structure

Ethacrynic acid Chemical Structure

CAS No. : 58-54-8

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Solid + Solvent
10 mM * 1 mL in DMSO
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100 mg USD 95 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

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Description

Ethacrynic acid has anti-inflammatory and anticancer activity. Ethacrynic acid is an orally active diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferase (GSTs) and Wnt signaling pathways. Ethacrynic acid is a radiosensitizer. Ethacrynic acid can inhibit airway smooth muscle (ASM) contraction in mice. Ethacrynic acid can increase the outflow of aqueous humor from the eye for the study of glaucoma[1][2][3][4][5][6][7][8][9].

IC50 & Target

L-type calcium channel

 

In Vitro

Ethacrynic acid (50 μM; 24 h) inhibits Wnt/β-catenin signaling in CLL cells[1].
Ethacrynic acid (1-100 μM; 48 h) is cytotoxic in CLL cells with an IC50 of 8.56 μM[1].
Ethacrynic acid (0.01-0.25 mmol/L; 30 min) increases aqueous humor outflow facility acutely in eye and the outflow rate increases from 28% to 105%[2].
Ethacrynic acid (10-100 μM; 30 min) can inhibit the activation of NF-κB pathway in RAW264.7 cells induced by LPS (100 ng/mL) and has anti-inflammatory activity[3].
Ethacrynic acid (20 μM/mL; 2 h) can increase the radiation intensity in MCF-7 cancer cells after radiation exposure[3].
Ethacrynic acid (100 μmol/L; 62.5-250 min) inhibits tracheal ring contraction induced by high -K+ (80 mmol/L) and acetylcholine (ACh, 100 µmol/L) in a dose-dependent manner with EC50 of 40.28 µmol/L and 56.22 µmol/L, respectively[8].
Ethacrynic acid (100 μmol/L; 500-2500 s) decreases the intracellular Ca2+ concentration induced by high -K+ and ACh from 0.40 to 0.16, 0.50 to 0.39, respectively[8].

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

RT-PCR[1]

Cell Line: Chronic lymphocytic leukemia (CLL)
Concentration: 1 μM, 10 μM, 100 μM
Incubation Time: 16 h
Result: Depressed the expression of LEF-1, Cyclin D1 and Fibronectin in a concentration-dependent manner.( LEF-1, cyclin D1 and fibronectin are established target genes of the Wnt/b-catenin pathway).

Western Blot Analysis[3]

Cell Line: RAW 264.7
Concentration: 10 μM, 20 μM, 50 μM, 100 μM ;Before LPS treatment (100 ng/mL; 1 h)
Incubation Time: 30 min
Result: Inhibited the expression of iNOS mRNA.
Inhibited degradation of IκBα and IκBβ.
In Vivo

Ethacrynic acid (450 μg/mouse; Oral gavage; Once daily for 60 days) can inhibit tumor growth in the mice[5].

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

Animal Model: Myeloma Balb/c mice model[5]
Dosage: 450 μg/mouse
Administration: Oral gavage (p.o.); Once daily for 60 days. After BALB/c mice were injected subcutaneously with 5 × 105 MPC11 myeloma cells.
Result: Significantly inhibited tumor growth.
Clinical Trial
Molecular Weight

303.14

Formula

C13H12Cl2O4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)COC1=CC=C(C(C(CC)=C)=O)C(Cl)=C1Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (329.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 27.5 mg/mL (90.72 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2988 mL 16.4940 mL 32.9881 mL
5 mM 0.6598 mL 3.2988 mL 6.5976 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, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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 (8.25 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 (8.25 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:  PBS

    Solubility: 1 mg/mL (3.30 mM); Clear 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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: 99.98%

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, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 3.2988 mL 16.4940 mL 32.9881 mL 82.4701 mL
5 mM 0.6598 mL 3.2988 mL 6.5976 mL 16.4940 mL
10 mM 0.3299 mL 1.6494 mL 3.2988 mL 8.2470 mL
15 mM 0.2199 mL 1.0996 mL 2.1992 mL 5.4980 mL
20 mM 0.1649 mL 0.8247 mL 1.6494 mL 4.1235 mL
25 mM 0.1320 mL 0.6598 mL 1.3195 mL 3.2988 mL
30 mM 0.1100 mL 0.5498 mL 1.0996 mL 2.7490 mL
40 mM 0.0825 mL 0.4124 mL 0.8247 mL 2.0618 mL
50 mM 0.0660 mL 0.3299 mL 0.6598 mL 1.6494 mL
60 mM 0.0550 mL 0.2749 mL 0.5498 mL 1.3745 mL
80 mM 0.0412 mL 0.2062 mL 0.4124 mL 1.0309 mL
DMSO 100 mM 0.0330 mL 0.1649 mL 0.3299 mL 0.8247 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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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.

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Ethacrynic acid
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