Microsomal epoxide hydrolase
Microsomal epoxide hydrolase (mEH/EPHX1) is a conserved α/β-hydrolase biotransformation enzyme that converts epoxides to diols and can detoxify or bioactivate diverse substrates[1]. Mechanistically, EPHX1 supports xenobiotic metabolism and also metabolizes the endocannabinoid 2-arachidonoylglycerol (2-AG) to arachidonic acid and glycerol, linking microsomal epoxide hydrolase activity to lipid signaling research[2]. In cardiovascular disease models, Ephx1/Ephx2 disruption reduced DHET formation, and double-knockout hearts showed better postischemic functional recovery than wild-type hearts, supporting experimental use of EPHX1 in epoxyeicosatrienoic acid metabolism studies[3]. Compared with soluble epoxide hydrolase EPHX2, EPHX1 shows slow EET hydrolysis in vitro but significantly contributes to EET hydrolysis in vivo through a coupled reaction with cytochrome P450[3]. Disease-oriented studies further connect EPHX1 mutations or polymorphic variants with cancer susceptibility, preeclampsia, and hypercholanemia-related transcriptional defects[1][4]. For experimental applications, 2-alkylthio acetamides provide low-nanomolar human mEH inhibitors, while ureas, amides, and amines established earlier inhibitor classes for probing microsomal epoxide hydrolase function[5][6].
References:
- [1]. Václavíková R, et al. Microsomal epoxide hydrolase 1 (EPHX1): Gene, structure, function, and role in human disease. Gene. 2015 Oct 15;571(1):1-8. [Content Brief]
- [2]. Nithipatikom K, Endsley M P, Pfeiffer A W, et al. A novel activity of microsomal epoxide hydrolase: metabolism of the endocannabinoid 2-arachidonoylglycerol[J]. Journal of lipid research, 2014, 55(10): 2093-2102. [Content Brief]
- [3]. Edin ML, et al. Epoxide hydrolase 1 (EPHX1) hydrolyzes epoxyeicosanoids and impairs cardiac recovery after ischemia. J Biol Chem. 2018 Mar 2;293(9):3281-3292. [Content Brief]
- [4]. Peng H, et al. Transcription of the Human Microsomal Epoxide Hydrolase Gene (EPHX1) Is Regulated by PARP-1 and Histone H1.2. Association with Sodium-Dependent Bile Acid Transport. PLoS One. 2015 May 20;10(5):e0125318. [Content Brief]
- [5]. Barnych B, et al. Development of potent inhibitors of the human microsomal epoxide hydrolase. Eur J Med Chem. 2020 May 1;193:112206. [Content Brief]
- [6]. Morisseau C, et al. Inhibition of microsomal epoxide hydrolases by ureas, amides, and amines. Chem Res Toxicol. 2001 Apr;14(4):409-15. [Content Brief]
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Microsomal epoxide hydrolase Related Products (1)
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sEH-IN-23
0 ImagesCat. No.: HY-182283sEH-IN-23 is a soluble epoxide hydrolase inhibitor with a IC50 of 0.8 nM against human sEH and 0.7 nM against murine sEH. sEH-IN-23 inhibits inflammatory factor production mediated by NF-κB activation, reactive oxygen species (ROS) generation, and the release of pro-inflammatory cytokines IL-1β, IL-6 and TNF-α. sEH-IN-23 exhibits anti-inflammatory activity in acute lung injury models. sEH-IN-23 can be used for the research of acute lung injury.
