Table 1.
Efficacy results in live cells or in vivo models of dual inhibitors/modulators.
| Target | Agent | Disease | species | Major outcomes | Reference |
|---|---|---|---|---|---|
| sEH/COX-2 (section 2.1.2) | PTUPB | Inflammatory Pain | Rat | Oral PTUPB reduced intraplantar LPS pain in von Frey assay | Hwang et al. 2011 |
| Kidney Disease | Rat | Dual COX-2/sEH inhibitor reduced renal damage and inflammation in ZDF Rats | Hye Khan et al. 2016 | ||
| Cancer | Mouse | Dual Inhibitor PTUPB inhibits Primary Tumor Growth and Metastasis. | Zhang et al. 2014 | ||
| Cancer | Glioblastoma cells, Mouse | PTUPB suppresses glioblastoma growth in vitro and in vivo | Li et al. 2017 | ||
| Mouse | PTUPB decreased fibrotic markers in liver injury | Harris et al. 2018 | |||
| Parkinson’s disease | Drosophila | Prevent the reduction of dopamine and its metabolites | Lakkappa et al. 2018 | ||
| sEH/FLAP (section 2.1.3) | diflapolin | Peritonitis | Mouse | Diflapolin blocked leukotriene formation and suppressed neutrophil infiltration | Garscha et al. 2017 |
| sEH/5-LOX (section 2.1.4) | Inflammatory Edema | Rat | Significant inhibition of the edema | Nandha et al. 2018 | |
| KM55 | LPS | THP-1, HUVEC cells | Significantly inhibited the LPS-induced adhesion of leukocytes to endothelial cells | Meirer et al. 2008 | |
| sEH/PPAR(section 2.2.1) | RB394 | ZSF1 Rat | Reduced blood pressure, blood glucose level, dyslipidemia and hypercholesteremia, as well as liver and kidney fibrosis | Hye Khan et al. 2018 | |
| Inflammatory Edema | Mouse | Superior anti-inflammatory properties in the zymosan-induced paw edema model | Schierle et al. 2018 | ||
| sEH/FXR (section 2.2.2) | FXR/sEH dual modulator | Inflammation | HEPG2, HuT-78 cells | Robustly repressed NF-κB in hepatocarcinoma cells and reduced the Pam3CSK4 stimulated release of TNFα from the T-cell line HuT-78 | Schmidt et al. 2017 |
| sEH/FAAH | FAAH/sEH dual inhibitor | A hit compound, t-TUCB, has been optimized through SAR study. The optimized compounds showed improved cross-species potencies against both FAAH and sEH. | Kodani et al. 2018 | ||
| sEH/C-RAF (section 2.2.4) | t-CUPM | pancreatic carcinoma | Mouse, PK03 cells | Inhibition of murine Pancreatic carcinoma growth in vitro and in vivo by t-CUPM | Liao et al. 2016 |