XCT-790
XCT-790 is a potent and selective inverse agonist ligand of the estrogen-related receptor alpha (ERRα).[1] Independent of its inhibition of ERRα, XCT-790 is a potent mitochondrial electron transport chain uncoupler. [2]
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| IUPAC name
(2E)-3-(4-{[2,4-bis(trifluoromethyl)benzyl]oxy}-3-methoxyphenyl)-2-cyano-N-[5-(trifluoromethyl)-1,3,4-thiadiazol-2-yl]acrylamide | |
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3D model (JSmol) |
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| ChEMBL | |
| ChemSpider | |
| ECHA InfoCard | 100.163.130  |
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CompTox Dashboard (EPA) |
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| Properties | |
| C23H13F9N4O3S | |
| Molar mass | 596.424949 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). | |
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| Infobox references | |
Mitochondrial electron transport chain uncoupling effect
XCT-790 has been shown to uncouple oxygen consumption from ATP production in mitochondria at very low, nanomolar-range doses independently of ERRα expression. Its effects are similar to proton ionophores such as FCCP, which disrupt mitochondrial transmembrane electrochemical gradients. This uncoupling leads to a fast drop in ATP production and, consequently, a prompt activation of AMPK.[2]
References
- Busch BB, Stevens WC Jr, Martin R, Ordentlich P, Zhou S, Sapp DW, Horlick RA, Mohan R; Stevens (November 2004). "Identification of a selective inverse agonist for the orphan nuclear receptor estrogen-related receptor alpha". J. Med. Chem. 47 (23): 5593–6. doi:10.1021/jm049334f. PMID 15509154.CS1 maint: multiple names: authors list (link)
- Eskiocak B; Aktar Ali; White MA (July 7, 2014). "The estrogen-related receptor α inverse agonist XCT 790 is a nanomolar mitochondrial uncoupler". Biochemistry. 53 (29): 4839–4846. doi:10.1021/bi500737n. PMC 4116149. PMID 24999922.
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