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GW6471

Cat. No. M2746

All AbMole products are for research use only, cannot be used for human consumption.

GW6471 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
2mg USD 48  USD48 In stock
5mg USD 72  USD72 In stock
10mg USD 108  USD108 In stock
50mg USD 435  USD435 In stock
100mg USD 645  USD645 In stock
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Quality Control & Documentation
Biological Activity

GW6471 completely inhibits GW409544-induced activation of PPARα with IC50 of 0.24 μM. GW6471 (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 (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. GW6471 (10 μM) abolishes the effect of fenofibrate (10 μM) or PPARα agonist WY14643 (50 μM), which raise levels of eNOS, NO, and BH4 in human umbilical vein endothelial cells.

Product Citations
Chemical Information
Molecular Weight 619.67
Formula C35H36F3N3O4
CAS Number 880635-03-0
Solubility (25°C) DMSO 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Omran Abu Aboud, et al. Am J Physiol Cell Physiol. PPARα inhibition modulates multiple reprogrammed metabolic pathways in kidney cancer and attenuates tumor growth

[2] Omran Abu Aboud, et al. PLoS One. Inhibition of PPARα induces cell cycle arrest and apoptosis, and synergizes with glycolysis inhibition in kidney cancer cells

[3] H Eric Xu, et al. Nature. Structural basis for antagonist-mediated recruitment of nuclear co-repressors by PPARalpha

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Keywords: GW6471 supplier, PPAR, inhibitors, activators

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