hseh

trans-AUCB (t-AUCB) is an effective and selective soluble epoxide hydrolase inhibitor, with IC50 values of 1.3 nM for hsEH, 8 nM for mouse sEH, and 8 nM for rat sEH.

N-(3-methoxybenzyl)-octadecanamide deverts from Maca (Lepidium meyenii Walp.).

AR-9281 (APAU) is a potent and selective inhibitor of soluble epoxide hydrolase (s-EH) potentially for the treatment of hypertension and type 2 diabetes

Soluble epoxide hydrolase inhibitor is a soluble epoxide hydrolase inhibitor (human soluble epoxide hydrolase (h-sEH) with pIC50 of 8.4).

Dual FAAH/sEH-IN-1 is a dual inhibitor of sEH (soluble epoxide hydrolase) (IC50: 9.6 nM) and FAAH (fatty acid amide hydrolase) (IC50: 7 nM) with high affinity and anti-inflammatory activity.

sEH-degrader-1 (Compound 8) acts as an effective inhibitor of sEH, exhibiting IC50 values of 3.8 nM for hsEH and 210 nM for msEH. Additionally, it proficiently degrades sEH in both mouse liver and brown adipose tissue.

sEH-IN-21 is an orally active inhibitor of sEH, exhibiting IC50 values of 0.1 nM for both hsEH and msEH. It significantly suppresses the NF-κB signaling pathway. sEH-IN-21 demonstrates potent anti-inflammatory activity by reducing IL-6 and TNF-α release and maintaining intestinal barrier integrity. It is applicable in research on inflammatory bowel disease (IBD).

PROTACsEH-degrader-3 (Compound 1a) is a targeted sEH PROTAC degrader that selectively degrades cytosolic sEH without affecting sEH in peroxisomes. It degrades sEH through a CRBN-dependent lysosomal pathway rather than the proteasomal pathway, with an IC50 of 0.8 nM for hsEH. Additionally, PROTACsEH-degrader-3 inhibits endoplasmic reticulum stress, making it useful for research on diseases related to inflammation, metabolic disorders, and other conditions associated with endoplasmic reticulum stress.

sEH/AChE-IN-3 (15) serves as a dual inhibitor targeting both soluble epoxide hydrolase (sEH) and acetylcholinesterase (AChE), demonstrating potent activity and the ability to cross the blood-brain barrier (BBB). It exhibits IC50 values of 0.4 nM for human sEH (hsEH), 1.94 nM for human AChE (hAChE), 615 nM for human butyrylcholinesterase (hBChE), 4.3 nM for mouse sEH (msEH), and 2.61 nM for mouse AChE (mAChE), indicating its efficacy across these enzymes.

sEH/AChE-IN-4 -15 is a potent, blood-brain barrier-penetrating dual inhibitor targeting soluble epoxide hydrolase (sEH) and acetylcholinesterase (AChE). It demonstrates notable inhibition efficacy, with IC50 values of 3.1 nM (hsEH), 1660 nM (hAChE), 179 nM (hBChE, human butyrylcholinesterase), 14.5 nM (msEH), and 102 nM (mAChE), indicating its significant inhibitory action across both targeted enzymes in human and mouse models.