Name: GSK3787
Price: 255.00 USD

- Overview
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    Background
    
    GSK3787 is a novel and irreversible antagonist of the peroxisome proliferator-activated receptor-β/δ (PPAR-β/δ) that covalently binds to a cysteine residue in the ligand-binding domain of PPAR- β/δ. Although it responses to ligand activation to modulate the association of both PPAR-β/δ and PPAR-γ coregulator peptides, GSK3787 exhibits considerably higher antagonism of PPAR-β/δ than that of PPAR-γ. Results of recent studies have shown that oral administration of GSK3787 results in the antagonism of GW0742-induced overexpression of Angptl4 and Adrp mRNA in wild-type mouse colon, which is correlated with reduced promoter occupancy of PPAR-β/δ on the Angptl4 and Adrp genes.
- Properties
  - Categories
    
    PPARβ/δ antagonist, novel and irreversible
    
    Alternative Name
    
    GSK-3787,GSK 3787; 4-chloro-N-[2-[5-(trifluoromethyl)pyridin-2-yl]sulfonylethyl]benzamide
    
    CAS Number
    
    188591-46-0
    
    Molecular Formula
    
    C15H12ClF3N2O3S
    
    Molecular Weight
    
    392.78
    
    Appearance
    
    A solid
    
    Purity
    
    99.72%
    
    Solubility
    
    insoluble in H2O; ≥15.8 mg/mL in DMSO; ≥2.89 mg/mL in EtOH with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    SMILES
    
    C1=CC(=CC=C1C(=O)NCCS(=O)(=O)C2=NC=C(C=C2)C(F)(F)F)Cl
    
    * For Research Use Only