| IUPAC name
|3D model (Jmol)||Interactive image|
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
|(what is ?)|
XCT790 is a potent and selective inverse agonist ligand of the estrogen-related receptor alpha. Independent of its inhibition of ERRα, XCT790 is a potent mitochondrial electron transport chain uncoupler.
Mitochondrial electron transport chain uncoupling effect
XCT790 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.
- 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.
- 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. PMID 24999922.