assay
≥95% (HPLC)
form
crystalline solid
solubility
DMSO: 20 mg/mL, methanol: soluble
General description
A cell-permeable, selective and irreversible PPARγ antagonist (IC50 = 3.3 nM, 32 nM, and 2 μM for PPARγ, PPARα, and PPARδ, 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-α (LXRα), retinoic acid receptor (RAR), retinoid X receptor-α (RXRα) and thyroid receptors α and β (TRα and TRβ).
Biochem/physiol Actions
Target IC50:3.3 nM, 32 nM, and 2 μM for PPARγ, PPARα, and PPARΔ
Preparation Note
Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Storage Class
10-13 - German Storage Class 10 to 13
Certificates of Analysis (COA)
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