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CAS No. 880635-03-0 (436159-64-7 deprecated)
GW 6471 is a potent antagonist of PPARα with IC50 of 0.24 μM.
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|Description||GW 6471 is a potent antagonist of PPARα with IC50 of 0.24 μM.|
GW6471 completely inhibits GW409544-induced activation of PPARα with IC50 of 0.24 μM. GW6471 at concentration ranging from 0.001-10 μM disrupts the interactions between PPAR and coactivator motifs derived from SRC-1 or CBP, but promotes the binding of the co-repressor motifs from SMRT or N-CoR. GW6471 adopts a U-shaped configuration and wraps around C276 of helix 3, destroys the integrity of the charge clamp but leaves sufficient space to accommodate the additional helical turn of the co-repressor motif in the PPAR/GW6471/SMRT complexes.  GW6471 at concentration of 10 μM significantly prevents cardiomyocyte differentiation and results in the reduced expression of cardiac sarcomeric proteins (ie α-actinin, troponin-T) and specific genes (ie α-MHC, MLC2v) in a time-dependent manner through inhibiting PPARα. 
|In vitro||DMSO||100 mg/mL (161.37 mM)|
|Ethanol||30 mg/mL (48.41 mM)|
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|CAS No.||880635-03-0 (436159-64-7 deprecated)|
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