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Beschreibung

Category: Inhibitors /// Appearance: White to Off-White Solid /// Application Notes: A cell-permeable, selective and irreversible PPARgamma antagonist (IC50 = 3.3 nM, 32 nM, and 2 µM for PPARgamma, PPARalpha, and PPARdelta, respectively). Reported to covalently modify a cysteine residue in the binding site of PPAR. At a concentration of 10 µM, also acts as an agonist of human pregnane X receptor (PXR) and farnesoid X receptor (FXR). Does not activate liver X receptor-a (LXRa), retinoic acid receptor (RAR), retinoid X receptor-a (RXRa) and thyroid receptors a and b (TRa and TRb /// References: Huang, J.T., et al.: Nature, 400, 378 (1999), Wilson, T.M., et al.: J. Med. Chem., 43, 527 (2000), Leesnitzer, L.M., et al.: Biochemistry, 41, 6640 (2002)