GSK-2256294A
(1R,3S)-N-(4-cyano-2-(trifluoromethyl)benzyl)-3-((4-methyl-6-(methylamino)-1,3,5-triazin-2-yl)amino)cyclohexane-1-carboxamide
CAS: 1142090-23-0
Molecular Formula: C21H24F3N7O
GSK-2256294A - Names and Identifiers
GSK-2256294A - Physico-chemical Properties
| Molecular Formula | C21H24F3N7O |
| Molar Mass | 447.46 |
| Density | 1.34±0.1 g/cm3(Predicted) |
| Solubility | DMSO: ≥ 47 mg/mL |
| pKa | 14.75±0.40(Predicted) |
| Storage Condition | -20℃ |
| Use | GSK2256294, also known as GSK2256294A, is a potent and selective sEH inhibitor, which is in investigation in patients with endothelial dysfunction or abnormal tissue repair, such as diabetes, wound healing or COPD. GSK2256294 exhibited potent cell-based activity, a concentration-dependent inhibition of the conversion of 14,15-EET to 14,15-DHET in human, rat and mouse whole blood in vitro, and a dose-dependent increase in the LTX/LTX diol ratio in rat plasma following oral administration. |
| Target | IC50: 27 pM (recombinant human sEH), 61 pM (rat sEH orthologs), 189 pM (murine sEH orthologs) |
GSK-2256294A - Reference
| Reference Show more | 1: Lazaar AL, Yang L, Boardley RL, Goyal NS, Robertson J, Baldwin SJ, Newby DE,Wilkinson IB, Tal-Singer R, Mayer RJ, Cheriyan J. Pharmacokinetics,pharmacodynamics and adverse event profile of GSK2256294, a novel soluble epoxidehydrolase inhibitor. Br J Clin Pharmacol. 2015 Dec 1. doi: 10.1111/bcp.12855.[Epub ahead of print] PubMed PMID: 26620151. 2: Podolin PL, Bolognese BJ, Foley JF, Long E 3rd, Peck B, Umbrecht S, Zhang X,Zhu P, Schwartz B, Xie W, Quinn C, Qi H, Sweitzer S, Chen S, Galop M, Ding Y,Belyanskaya SL, Israel DI, Morgan BA, Behm DJ, Marino JP Jr, Kurali E, BarnetteMS, Mayer RJ, Booth-Genthe CL, Callahan JF. In vitro and in vivo characterizationof a novel soluble epoxide hydrolase inhibitor. Prostaglandins Other LipidMediat. 2013 Jul-Aug;104-105:25-31. doi: 10.1016/j.prostaglandins.2013.02.001.Epub 2013 Feb 19. PubMed PMID: 23434473. 3: Morgan LA, Olzinski AR, Upson JJ, Zhao S, Wang T, Eisennagel SH, Hoang B,Tunstead JR, Marino JP Jr, Willette RN, Jucker BM, Behm DJ. Soluble epoxidehydrolase inhibition does not prevent cardiac remodeling and dysfunction afteraortic constriction in rats and mice. J Cardiovasc Pharmacol. 2013Apr;61(4):291-301. doi: 10.1097/FJC.0b013e31827fe59c. PubMed PMID: 2323284 |
GSK-2256294A - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.235 ml | 11.174 ml | 22.349 ml |
| 5 mM | 0.447 ml | 2.235 ml | 4.47 ml |
| 10 mM | 0.223 ml | 1.117 ml | 2.235 ml |
| 5 mM | 0.045 ml | 0.223 ml | 0.447 ml |
Last Update：2024-01-02 23:10:35
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