Epoxide Hydrolase Inhibitor

sEH inhibitor-3 (compound 35) is a potent and orally active soluble epoxide hydrolase (sEH) inhibitor with a K_i of 0.75 nM for human sEH.

sEH inhibitor-14 (compound 33) is a benzoxazolone-5-urea analogue. In addition, sEH inhibitor-14 is a soluble Epoxide Hydrolase (sEH) inhibitor (IC₅₀=0.39 nM).

sEH inhibitor-12 (compound 34) is a sEH inhibitor with an IC₅₀ value of 0.7 μM. sEH inhibitor-12 inhibits the 5-lipoxygenase-activating protein (FLAP)-mediated leukotriene (LT) biosynthesis with an IC₅₀ value of 2.9 μM. sEH inhibitor-12 can be used for the research of inflammation.

sEH/HDAC6-IN-1 (compound M9) is a selective, orally active dual inhibitor for sEH and HDAC6, with IC₅₀s of 2 nM, 0.72 nM and 5 nM, for human sEH, murine sEH and HDAC6, respectively. sEH/HDAC6-IN-1 reveals analgesic and anti-inflammatory effects.

sEH/HDAC6-IN-2 is a potent dual soluble epoxide hydrolase (sEH) and HDAC6 inhibitor with IC₅₀s of 0.9 nM, 46.8 nM, and 8 nM for human sEH, mouse sEH, and HDAC6, respectively. sEH/HDAC6-IN-2 can be used for the study of inflammatory pain.

Moracin M 3’-O-β-glucopyranoside is found in Morus alba. Moracin M 3’-O-β-glucopyranoside is a sEH inhibitor (IC₅₀: 7.7 µM). Moracin M 3’-O-β-glucopyranoside exhibits anti-inflammatory activity.

sEH-IN-1 (example 67) is a soluble epoxide hydrolase (sEH) inhibitor. sEH-IN-1 can be used in the research of sEH-mediated diseases such as hypertension, cardiovascular disease, inflammation, diabetes, and so on.

SP-C01 is an orally active soluble epoxide hydrolase (sEH) inhibitor and partial PPARγ agonist. SP-C01 can inhibit Ser273 phosphorylation.

sEH inhibitor-13 (compound 43) is a potent soluble epoxide hydrolase (sEH) inhibitor, with an IC₅₀ of 0.4 μM.

sEH-IN-22 (Compound 1) is a soluble epoxide hydrolase (sEH) inhibitor (IC₅₀ = 1.1 μM) found in Rubia philippinensis. sEH-IN-22 exhibits anti-inflammatory, analgesic and blood pressure-regulating effects. sEH-IN-22 can be used for the researches of inflammation, neurological and cardiovascular disease.

SH-11037 is a potent inhibitor of soluble epoxide hydrolase (sEH) and docks to the substrate binding cleft in the sEH hydrolase domain. SH-11037 dose-dependently suppresses angiogenesis in the choroidal sprouting assay ex vivo and inhibited ocular developmental angiogenesis in zebrafish larvae. SH-11037 reduces choroidal neovascularisation lesion volume in the laser-induced CNV mouse model. SH-11037 synergises with anti-VEGF treatments in vitro and in vivo. SH-11037 induces G2/M phase blockade and retains retinal endothelial cell viability at active concentrations without overt toxicity. SH-11037 can be used for the research of retinal neovascularization and ocular neovascularization.

mPGES-1/sEH-IN-1 (compound 1f) is an inhibitor of sEH with IC₅₀ value of 5 μM. mPGES-1/sEH-IN-1 shows antitumor activity with IC₅₀ value of 25 µM via inhibts mPGES‐1.

sEH-H ligand 1 is a PROTAC target protein ligand that can be used to synthesize PROTAC sEH degrader-2 (HY-174443).

sEH-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.

FZQ-21 (Compound 70P) is a soluble epoxide hydrolase (sEH) inhibitor, with an IC₅₀ of 4 nM. FZQ-21 exhibits equal IC₅₀ (1.5 nM) on inhibiting human sEH as EC5026 (HY-135653) (1.7 nM). FZQ-21 can be used for research of sepsis.

Moracin M 3'-O-β-D-glucopyranoside is a natural product with multiple activities such as hypoglycemic and antitumor effects. Moracin M 3'-O-β-D-glucopyranoside acts as an inhibitor of mushroom tyrosinase with an IC₅₀ of 127.5 μM, and also functions as an inhibitor of soluble epoxide hydrolase with an IC₅₀ of 7.7 μM. Moracin M 3'-O-β-D-glucopyranoside can be used in studies related to hyperglycemia and skin tumors.

5-LOX/sEH-IN-1 (Compound 8o) is a dual 5-LOX/sEH-IN-1 inhibitor with cardioprotective effects, exhibiting IC₅₀ values of 3.05 μM and 2.20 nM respectively, and 5-LOX/sEH-IN-1 can also inhibit the activity of COX-2 (IC₅₀=10.50 μM). 5-LOX/sEH-IN-1 has analgesic and anti-inflammatory effects, while reducing ulcer pathogenicity, and can be used to develop anti-inflammatory agents with fewer gastrointestinal and cardiovascular side effects.

sEH inhibitor-2 (compound 5l) is an orally active (predicted percentage absorption: 71.2-88.4%) soluble epoxide hydrolase (sEH) inhibitor, with an IC₅₀ of 0.9 nM. sEH inhibitor-2 can maintain epoxyeicosatrienoic acids (EETs) serum level in high concentrations. sEH inhibitor-2 can be used in study of cardiovascular protection.

sEH/AChE-IN-3 (compound (−)-15) is a potent and BBB-penetrated dual inhibitor of sEH (soluble epoxide hydrolase) and AChE (acetylcholinesterase), with IC₅₀ values of 0.4 nM (hsEH), 1.94 nM (hAChE), 615 (hBChE, human butyrylcholinesterase), 4.3 nM (msEH), and 2.61 nM (mAChE), respectively.

4H-Tomentosin is a mixed-competitive type soluble epoxide hydrolase (sEH) inhibitor with an IC₅₀ of 6.84 μM and a K_i of 7.02 μM. 4H-Tomentosin interacts with sEH by forming hydrogen bonds with Tyr343, Ile363, and Tyr383.