Soluble epoxide hydrolase inhibitor

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

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

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.

(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.

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

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.

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.

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.

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

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.

SWE101 is a potent human and rat soluble epoxide hydrolase (sEH)-P inhibitor(IC50s of 4 μM and 2.8 μM, respectively).

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

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.

UC-1728 (t-TUCB) is an effective rabbit soluble epoxide hydrolase inhibitor (IC50: 2 nM on rabbit liver).

DJ-53 (compound 68) is an orally active, phenyl-quinoline-based soluble epoxide hydrolase inhibitor.

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.

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.

sEH-IN-12 is an effective inhibitor of the enzyme soluble epoxide hydrolase (sEH).

N-Desbutyl dronedarone is an active metabolite of the antiarrhythmic agent dronedarone .1,2,3It is formed from dronedarone by cytochrome P450s (CYPs) and monoamine oxidase (MAO) in human hepatocyte preparations.4N-Desbutyl dronedarone inhibits the binding of 3,3',5-triiodo-L-thyronine to the thyroid hormone receptors TRα1and TRβ1(IC50s = 59 and 280 μM for the chicken and human receptors, respectively).1It inhibits CYP2J2-mediated formation of 14,15-EET from arachidonic acid and soluble epoxide hydrolase-mediated formation of 14,15-DHET from 14,15-EET (IC50s = 1.59 and 2.73 μM, respectively, in cell-free assays).2N-Desbutyl dronedarone decreases intracellular ATP levels in H9c2 rat cardiomyocytes (IC50= 1.07 μM) and inhibits mitochondrial complex I, also known as NADH dehydrogenase, and mitochondrial complex II, also known as succinate dehydrogenase, activities in isolated rat heart mitochondria (IC50s = 11.94 and 24.54 μM, respectively).3 1.Van Beeren, H.C., Jong, W.M.C., Kaptein, E., et al.Dronerarone acts as a selective inhibitor of 3,5,3'-triiodothyronine binding to thyroid hormone receptor-α1: in vitro and in vivo evidenceEndocrinology144(2)552-558(2003) 2.Karkhanis, A., Tram, N.D.T., and Chan, E.C.Y.Effects of dronedarone, amiodarone and their active metabolites on sequential metabolism of arachidonic acid to epoxyeicosatrienoic and dihydroxyeicosatrienoic acidsBiochem. Pharmacol.146188-198(2017) 3.Karkhanis, A., Leow, J.W.H., Hagen, T., et al.Dronedarone-induced cardiac mitochondrial dysfunction and its mitigation by epoxyeicosatrienoic acidsToxicol. Sci.163(1)79-91(2018) 4.Klieber, S., Arabeyre-Fabre, C., Moliner, P., et al.Identification of metabolic pathways and enzyme systems involved in the in vitro human hepatic metabolism of dronedarone, a potent new oral antiarrhythmic drugPharmacol. Res. Perspec.2(3)e00044(2014)

sEH inhibitor-6 (Compound 3g) is a highly potent soluble epoxide hydrolase (sEH) inhibitor, exhibiting an IC50 value of 0.5 nM [1].

SEH inhibitor-2 (compound 5l) is a soluble epoxide hydrolase (sEH) inhibitor with oral activity (IC50=0.9 nM), and the predicted oral absorption percentage is 71.2-88.4%. SEH inhibitor-2 can maintain a high concentration of eicosanoic acid (EETs) in serum. SEH inhibitor-2 has research value in cardiovascular protection.

sEH inhibitor-3 (compound 35) is a potent, orally active inhibitor of soluble epoxide hydrolase (sEH), acting on human sEH with a Ki of 0.75 nM.

COX-2 sEH-IN-1 is an orally active dual inhibitor of COX-2 (IC50: 1.24 μM) and sEH (IC50: 0.40 μM), a soluble epoxide hydrolase. COX-2 sEH-IN-1 increases anti-inflammatory effects and significantly reduces cardiovascular risk.