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GW6471

Cat. No. M2746

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GW6471 Structure
Size Price Availability Quantity
10mM*1mL in DMSO USD 90 In stock
2mg USD 38 In stock
5mg USD 56 In stock
10mg USD 98 In stock
50mg USD 388 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
Protocol (for reference only)
Cell Experiment
Cell lines MDA-MB-231
Preparation method To analyze cell viability, dissociated mammospheres were plated at 1 × 10^6 cells/mL and after 72 h hours were treated with different concentrations of GW6471 for 72 h. Then, the MTS assay was performed.
Concentrations 4, 8, 16 μM
Incubation time 72 h
Animal Experiment
Animal models Male Balb/c mice
Formulation DMSO 50 % in saline
Dosages 10 mg/kg
Administration Intraperitoneally injected
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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  Catalog
Abmole Inhibitor Catalog




Keywords: GW6471 supplier, PPAR, inhibitors, activators

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