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GSK 2256294A
- GSK 2256294
Axon 2220
CAS:
1142090-23-0
- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C21H24F3N7O
- MW: 447.46
Description
GSK 2256294A is a potent, reversible, tight binding inhibitor of isolated recombinant human sEH (IC50 value 27 pM), and displays potent inhibition against the rat (IC50 = 61 pM) and murine (IC50 = 189 pM) orthologs of sEH. GSK 2256294A also displays potent cellular inhibition (IC50 = 0.66 nM) of sEH in a cell line transfected with the human sEH enzyme.The selectivity of the compound has been demonstrated by testing against a large panel of enzymes, receptors and ion channels, including the phosphatase activity of EPHX2.
More Information
| Parent CAS No. | 1142090-23-0 |
|---|---|
| Chemical Name | (1R,3S)-N-(4-cyano-2-(trifluoromethyl)benzyl)-3-(4-methyl-6-(methylamino)-1,3,5-triazin-2-ylamino)cyclohexanecarboxamide |
| SMILES | C1(C#N)C=CC(CNC(=O)[C@@H]2CCC[C@H](NC3N=C(NC)N=C(C)N=3)C2)=C(C(F)(F)F)C=1 |&1:10,14,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C21H24F3N7O/c1-12-28-19(26-2)31-20(29-12)30-16-5-3-4-14(9-16)18(32)27-11-15-7-6-13(10-25)8-17(15)21(22,23)24/h6-8,14,16H,3-5,9,11H2,1-2H3,(H,27,32)(H2,26,28,29,30,31)/t14-,16+/m1/s1 |
| InChiKey | LQHDJQIMETZMPH-ZBFHGGJFSA-N |
| CID | 59448236 |
| Short Description | sEH inhibitor |
References
- P.L. Podolin et al. In vitro and in vivo characterization of a novel soluble epoxide hydrolase inhibitor. Prostaglandins Other Lipid Mediat. 2013, 104-105, 25-31.
- L.A. Morgan et al. Soluble epoxide hydrolase inhibition does not prevent cardiac remodeling and dysfunction after aortic constriction in rats and mice. J. Cardiovasc. Pharmacol. 2013, 61, 291-301.
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