Biological Activity
Potent soluble epoxide hydrolase (sEH) inhibitor (IC50 values are 1.1 and 2.1 nM for murine and human receptor, respectively). Inhibits MAPK and NF-κB signaling, as well as reducing ER stress and cell death in models of pancreatitis. Exhibits antidepressant effects in a social defeat stress model. Orally bioavailable and brain penetrant.
Technical Data
| M. Wt | 359.34 |
| Formula | C16H20F3N3O3 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1222780-33-7 |
| PubChem ID | 44142782 |
| InChI Key | AAJMQTLFRTZCJK-UHFFFAOYSA-N |
| Smiles | CCC(N1CCC(NC(NC2=CC=C(C=C2)OC(F)(F)F)=O)CC1)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 35.93 | 100 | |
| ethanol | 17.97 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 359.34. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.78 mL | 13.91 mL | 27.83 mL |
| 5 mM | 0.56 mL | 2.78 mL | 5.57 mL |
| 10 mM | 0.28 mL | 1.39 mL | 2.78 mL |
| 50 mM | 0.06 mL | 0.28 mL | 0.56 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Ren et al (2016) Gene deficiency and pharmacological inhibition of soluble epoxide hydrolase confers resilience to repeated social defeat stress. Proc.Natl.Acad.Sci.U.S.A. 113 E1944 PMID: 26976569
Bettaieb et al (2015) Soluble epoxide hydrolase pharmacological inhibition ameliorates experimental acute pancreatitis in mice. Mol.Pharmacol. 88 281 PMID: 25993999
Rose et al (2010) 1-Aryl-3-(1-acylpiperidin-4-yl)urea inhibitors of human and murine soluble epoxide hydrolase: structure-activity relationships, pharmacokinetics, and reduction of inflammatory pain. J.Med.Chem. 53 7067 PMID: 20812725
Keywords: TPPU, supplier, potent, soluble, epoxide, hydrolase, inhibitors, inhibits, brain, penetrant, orally, bioavailable, antidepressant, anti-inflammatory, Other, Hydrolases, Other, Hydrolases, Tocris Bioscience
