Ethacrynic acidEthacrynic acid
MedChemExpress (MCE)
HY-B1640
58-54-8
Etacrynic acid
99.90%
4°C, protect from light *In solvent : -80°C, 1 year
-20°C, 6 months (protect from light)
Room temperature in continental US
may vary elsewhere.
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.
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].
Ethacrynic acid (450 μg/mouse
Oral gavage
Once daily for 60 days) can inhibit tumor growth in the mice[5].
L-type calcium channel
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[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].
