XCT-790
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Preferred IUPAC name (2E)-3-(4-{[2,4-Bis(trifluoromethyl)phenyl]methoxy}-3-methoxyphenyl)-2-cyano-N-[5-(trifluoromethyl)-1,3,4-thiadiazol-2-yl]prop-2-enamide | |
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ECHA InfoCard | 100.163.130 |
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Properties | |
Chemical formula | 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). N verify (what is YN ?) Infobox references |
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]
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.
{{cite journal}}
: CS1 maint: multiple names: authors list (link) - ^ a b 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.
External links
- XCT790 at the U.S. National Library of Medicine Medical Subject Headings (MeSH)
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- Agonists: 6,3′,4′-Trihydroxyflavone
- Biochanin A
- Bisphenol AF
- Cholesterol
- Daidzein
- Genistein
- SLU-PP-332
- Antagonists: Diethylstilbestrol
- XCT-790
- Agonists: DY-131 (GSK-9089)
- GSK-4716 (GW-4716)
- SLU-PP-332
- Agonists: Bisphenol A
- DY-131 (GSK-9089)
- GSK-4716 (GW-4716)
- SLU-PP-332
- Antagonists: 4-Hydroxytamoxifen (afimoxifene)
- Diethylstilbestrol
- See also
- Receptor/signaling modulators
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