epoxide hydrolase

Epoxide hydrolase, an enzyme responsible for catalyzing the reaction of epoxides with water to convert epoxy groups into diols, plays a crucial role in the metabolism of environmental pollutants and lipids. It is instrumental in detoxification, inflammatory responses, and regulating the health of the cardiovascular system. Additionally, Epoxide hydrolase is used in asymmetric catalytic reactions, such as the asymmetric ring-opening of epoxides, which are important for the synthesis of chiral pharmaceutical molecules.

sEH Inhibitor-16, a potent soluble epoxide hydrolase (sEH) inhibitor, exhibits an IC50 of 2 nM. It diminishes inflammatory damage associated with cerulein-induced acute pancreatitis (AP) in mice, making it suitable for inflammation and immunology research [1].

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 inhibitor-7 is a soluble epoxide hydrolase (sEH) inhibitor that inhibits sEH in human and mouse with IC 50 s of 6.2 μM and 0.15 μM, respectively. sEH inhibitor-7 is associated with anti-inflammatory active molecules.

VU534 is a NAPE-PLD agonist with an EC50 of 0.30 μM.VU534 is a dual inhibitor of FAAH and sEH, with an IC50 of 1.2 μM for sEH.VU534 is used in diseases related to cardiometabolism.

beta-Amyrin acetate inhibits HMG-CoA Reductase (HMGCR) and sEH activity with IC50 of 3.4 μM. beta-Amyrin acetate has anti-inflammatory, antifungal, antioxidant, and anti-hyperlipidemic activities.

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

Soluble epoxide hydrolase (sEH) PROTAC 1a is a proteolysis-targeting chimera (PROTAC) comprising a cereblon ligand linked to the sEH inhibitor t-TUCB via a linker, promoting selective sEH degradation and inhibiting its hydrolase activity (IC50 = 0.8 nM) significantly more than its phosphatase activity (IC50 = >10,000 nM). This compound preferentially targets cytosolic sEH for lysosomal rather than proteasomal degradation. Furthermore, it mitigates thapsigargin-induced upregulation of phosphorylated inositol-requiring enzyme 1α (IRE1α) and X-box binding protein 1 (XBP1) splicing in HepG2 and 293T cells, thereby reducing endoplasmic reticulum stress.

sEH inhibitor-19 (Compound (R)-14i) is an orally active soluble epoxide hydrolase (sEH) inhibitor with an IC50 of 1.2 nM. This compound suppresses the expression of TNF-α and IL-6 and exhibits anti-inflammatory effects in mouse models of acute pancreatitis and Carrageenan-induced edema.

mPGES-1 sEH-IN-1 (compound 1f) is an sEH inhibitor with an IC50 value of 5 μM. It also exhibits antitumor activity by inhibiting mPGES-1, with an IC50 value of 25 µM.

EC5026 (BPN-19186) has the potential to relieve pain by stabilizing natural analgesic and anti-inflammatory mediators.

(Rac)-EC5026 ((Rac)-BPN-19186) is a potent piperidine inhibitor of soluble epoxide hydrolase (sEH) with a Ki of 0.06 nM, useful for research on Parkinson's disease and dementia with Lewy Bodies (DLB) [1].

N,N'-Dicyclohexylurea (AURORA KA-3582) is a soluble epoxide hydrolase (sEH) inhibitor.

Valpromide (Dipropylacetamide) is a carboxamide derivative of valproic acid, used in the treatment of epilepsy and some affective disorders.

1, 3-Diphenylurea is involved with Epoxide hydrolase activity.

Diflapolin is a highly active dual 5-lipoxygenase-activating protein (FLAP) and soluble epoxide hydrolase (sEH) inhibitor, exhibiting marked anti-inflammatory efficacy and high target selectivity.

AUDA is an inhibitor of sEH(IC50 values of 18 and 69 nM for the mouse and human enzymes, respectively)

CAY10640 (sEH inhibitor-1) is a potent, orally active, water-soluble epoxide hydrolase (sEH) inhibitor that inhibits sEH in humans and mice with IC50s of 0.4 and 5.3 nM, respectively.

BI-1935 is an inhibitor of soluble epoxide hydrolase (sEH). For diseases related to cardiovascular disease.

ARM1 is a potent inhibitor of aminopeptidase and epoxide hydrolase. The IC50 values are 7.61 µM for aminopeptidase and 12.4 µM for epoxide hydrolase.

CUDA is an effective soluble cyclohydrolase inhibitor with IC50 of 11.1 nM and 112 nM for mouse sEH and human sEH, respectively. CUDA selectively increases the activity of peroxisome proliferator-activated receptor (PPAR) alpha. CUDA may be valuable for the study of cardiovascular diseases.

GSK2256294A (GSK 2256294) is potent, selective inhibitor of recombinant human, rat and mouse sEH with IC50 of 27 pM, 61 pM and 189 pM, respectively.

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.

LQ-38 is an orally active, soluble epoxide hydrolase (sEH) inhibitor with an IC50 value of 5.2 nM. It has shown anti-inflammatory activity in rat foot edema models and in mouse models of acute pancreatitis, and exhibits analgesic effects in acetic acid-induced mouse writhing models.