Ethacrynic acid (Synonyms: Etacrynic acid)

Name: Ethacrynic acid
Brand: MedChemExpress
SKU: HY-B1640
Rating: 5.0 (4 reviews)

Cat. No.: HY-B1640 Purity: 99.90%: FAQs
Data Sheet SDS COA Handling Instructions

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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

CAS No. : 58-54-8

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 61	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 61	In-stock	Estimated Time of Arrival: December 31
Solid
50 mg	USD 55	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 95	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 4 publication(s) in Google Scholar

Other Forms of Ethacrynic acid:

4 Publications Citing Use of MCE Ethacrynic acid

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

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nNOS iNOS eNOS

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

L-type calcium channel

Cellular Effect

Cell Line	Type	Value	Description	References
CHO-K1	EC₅₀	56 μM Compound: 1	Cytotoxicity against CHO-K1 cells by Alamar blue assay Cytotoxicity against CHO-K1 cells by Alamar blue assay	[PMID: 16962325]
HCT-116	IC₅₀	30.22 μM Compound: EA	Cytotoxic activity against human HCT116 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Cytotoxic activity against human HCT116 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 27156773]
HCT-116	IC₅₀	75 μM Compound: 1; EA	Antiproliferative activity against human HCT116 cells after 24 to 72 hrs by MTS assay Antiproliferative activity against human HCT116 cells after 24 to 72 hrs by MTS assay	[PMID: 27448922]
HL-60	IC₅₀	38 μM Compound: 1; EA	Cytotoxicity against human HL60 cells assessed as reduction in cell viability after 24 hrs by MTS assay Cytotoxicity against human HL60 cells assessed as reduction in cell viability after 24 hrs by MTS assay	[PMID: 27448922]
HL-60	GI₅₀	44.2 μM Compound: EA	Growth inhibition of human HL60 cells after 72 hrs by trypan blue staining Growth inhibition of human HL60 cells after 72 hrs by trypan blue staining	[PMID: 22370342]
HL-60	GI₅₀	44.2 μM Compound: EA	Antiproliferative activity against human HL60 cells after 72 hrs Antiproliferative activity against human HL60 cells after 72 hrs	[PMID: 17287120]
HL-60	GI₅₀	45 μM Compound: EA	Growth inhibition of human HL60 cells by hemocytometry Growth inhibition of human HL60 cells by hemocytometry	[PMID: 20055416]
HL-60	IC₅₀	46 μM Compound: 1; EA	Antiproliferative activity against human HL60 cells after 24 to 72 hrs by MTS assay Antiproliferative activity against human HL60 cells after 24 to 72 hrs by MTS assay	[PMID: 27448922]
HT-1080	IC₅₀	54.53 μM Compound: EA	Cytotoxic activity against human HT1080 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Cytotoxic activity against human HT1080 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 27156773]
HT-29	IC₅₀	62.39 μM Compound: EA	Cytotoxic activity against human HT-29 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Cytotoxic activity against human HT-29 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 27156773]
KB	IC₅₀	11 μM Compound: 1; EA	Antiproliferative activity against human KB cells after 24 to 72 hrs by MTS assay Antiproliferative activity against human KB cells after 24 to 72 hrs by MTS assay	[PMID: 27448922]
MCF7	IC₅₀	28.92 μM Compound: EA	Cytotoxic activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Cytotoxic activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 27156773]
MCF7	IC₅₀	41 μM Compound: 1; EA	Antiproliferative activity against human MCF7 cells after 24 to 72 hrs by MTS assay Antiproliferative activity against human MCF7 cells after 24 to 72 hrs by MTS assay	[PMID: 27448922]
MDA-MB-231	IC₅₀	45.24 μM Compound: EA	Cytotoxic activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Cytotoxic activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 27156773]
MDA-MB-468	IC₅₀	81.45 μM Compound: EA	Cytotoxic activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Cytotoxic activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 27156773]
NCI-H1299	IC₅₀	44.29 μM Compound: EA	Cytotoxic activity against human H1299 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Cytotoxic activity against human H1299 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 27156773]
OVCAR-8	IC₅₀	72 μM Compound: 1; EA	Antiproliferative activity against human OVCAR8 cells after 24 to 72 hrs by MTS assay Antiproliferative activity against human OVCAR8 cells after 24 to 72 hrs by MTS assay	[PMID: 27448922]
PC-3	IC₅₀	75 μM Compound: 1; EA	Antiproliferative activity against human PC3 cells after 24 to 72 hrs by MTS assay Antiproliferative activity against human PC3 cells after 24 to 72 hrs by MTS assay	[PMID: 27448922]
SF-188	IC₅₀	31.65 μM Compound: EA	Cytotoxic activity against human SF188 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Cytotoxic activity against human SF188 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 27156773]
SK-BR-3	IC₅₀	34.21 μM Compound: EA	Cytotoxic activity against human SKBR3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Cytotoxic activity against human SKBR3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 27156773]
SK-OV-3	IC₅₀	> 100 μM Compound: 1; EA	Antiproliferative activity against human SKOV3 cells after 24 to 72 hrs by MTS assay Antiproliferative activity against human SKOV3 cells after 24 to 72 hrs by MTS assay	[PMID: 27448922]
SW480	IC₅₀	32.7 μM Compound: 1	Inhibition of Wnt/beta-casein signaling in human SW480 cells by fluorimetry Inhibition of Wnt/beta-casein signaling in human SW480 cells by fluorimetry	[PMID: 19121941]

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.

58-54-8

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
10 mM	0.3299 mL	1.6494 mL	3.2988 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (8.25 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.

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)

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%

Select Batch:

Data Sheet (280 KB) SDS (393 KB)

COA (246 KB)

Handling Instructions (2659 KB)

References

[1]. Lu D, et al. Ethacrynic acid exhibits selective toxicity to chronic lymphocytic leukemia cells by inhibition of the Wnt/beta-catenin pathway. PLoS One. 2009 Dec 14;4(12):e8294. [Content Brief]

[2]. Liang LL, et al. Ethacrynic acid increases facility of outflow in the human eye in vitro. Arch Ophthalmol. 1992 Jan;110(1):106-9. [Content Brief]

[3]. Han Y,et al. Ethacrynic acid inhibits multiple steps in the NF-kappaB signaling pathway. Shock. 2005 Jan;23(1):45-53. [Content Brief]

[4]. Khil MS, et al. Ethacrynic acid: a novel radiation enhancer in human carcinoma cells. Int J Radiat Oncol Biol Phys. 1996 Jan 15;34(2):375-80. [Content Brief]

[5]. Kim Y, et al. In vivo efficacy of the diuretic agent ethacrynic acid against multiple myeloma. Leuk Res. 2012 May;36(5):598-600. [Content Brief]

[6]. Li XQ, et al. Metabolism of Strained Rings: Glutathione S-transferase-Catalyzed Formation of a Glutathione-Conjugated Spiro-azetidine without Prior Bioactivation. Drug Metab Dispos. 2019 Nov;47(11):1247-1256. [Content Brief]

[7]. Harada T, et al. Ethacrynic acid decreases expression of proinflammatory intestinal wall cytokines and ameliorates gastrointestinal stasis in murine postoperative ileus. Clinics (Sao Paulo). 2018 Oct 18;73:e332. [Content Brief]

[8]. Zhao XX, et al. [Ethacrynic acid inhibits airway smooth muscle contraction in mice]. Sheng Li Xue Bao. 2019 Dec 25;71(6):863-873. Chinese. PMID: 31879742. [Content Brief]

[9]. Byun HJ, Kang KJ, Park MK, Lee HJ, Kang JH, Lee EJ, Kim YR, Kim HJ, Kim YW, Jung KC, Kim SY, Lee CH. Ethacrynic Acid Inhibits Sphingosylphosphorylcholine-Induced Keratin 8 Phosphorylation and Reorganization via Transglutaminase-2 Inhibition. Biomol Ther (Seoul). 2013 Sep 30;21(5):338-42. [Content Brief]

[10].

Complete Stock Solution Preparation Table

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.

Ethacrynic acid Related Classifications

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Ethacrynic acid (Synonyms: Etacrynic acid)

Customer Review

Other Forms of Ethacrynic acid:

4 Publications Citing Use of MCE Ethacrynic acid

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Complete Stock Solution Preparation Table

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Ethacrynic acid (Synonyms: Etacrynic acid)

Customer Review

Other Forms of Ethacrynic acid:

Ethacrynic acid Related Antibodies

4 Publications Citing Use of MCE Ethacrynic acid

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All NF-κB Isoform Specific Products:

View All Calcium Channel Isoform Specific Products:

View All NO Synthase Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Ethacrynic acid Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

Ethacrynic acid Related Classifications

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