| Identification | Back Directory | [Name]
GW 6471 | [CAS]
880635-03-0 | [Synonyms]
GW 6471
GW 6471 USP/EP/BP
N-((2S)-2-(((1Z)-1-METHYL-3-OXO-3-(4-(TRIFLUOROMETHYL)PHENYL)PROP-1-ENYL)AMINO)-3-(4-(2-(5-METHYL-2-PHENYL-1,3-OXAZOL-4-YL)ETHOXY)PHENYL)PROPYL)PROPANAMIDE
Propanamide, N-[(2S)-2-[[(1Z)-1-methyl-3-oxo-3-[4-(trifluoromethyl)phenyl]-1-propen-1-yl]amino]-3-[4-[2-(5-methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]propyl]-
[(2S)-2-[[(1Z)-1-METHYL-3-OXO-3-[4-(TRIFLUOROMETHYL)PHENYL]-1-PROPENYL]AMINO]-3-[4-[2-(5-METHYL-2-PHENYL-4-OXAZOLYL)ETHOXY]PHENYL]PROPYL]-CARBAMIC ACID ETHYL ESTER | [Molecular Formula]
C35H36F3N3O4 | [MDL Number]
MFCD07784503 | [MOL File]
880635-03-0.mol | [Molecular Weight]
619.67 |
| Questions And Answer | Back Directory | [Uses]
GW 6471 is a potent antagonist of PPARα with IC50 of 0.24 μM. | [In vitro]
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. [1] 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.
| [Targets]
PPARα |
| Chemical Properties | Back Directory | [density ]
1.204±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: 15 mg/mL
| [form ]
solid
| [pka]
15.90±0.46(Predicted) | [color ]
off-white
|
| Hazard Information | Back Directory | [General Description]
GW6471 prevents apoptosis and cell cycle arrest at G0/G1 in renal cell carcinoma. It reduces enhanced fatty acid oxidation and oxidative phosphorylation associated with glycolysis inhibition. | [Biochem/physiol Actions]
GW6471 is a PPARα antagonist, which completely inhibits GW409544-induced activation of PPARα with an IC50 = 0.24 μM. GW6471 induces a PPARα conformation that interacts efficiently with co-repressors. | [storage]
Store at +4°C |
|
| Company Name: |
Sigma-Aldrich
|
| Tel: |
021-61415566 800-8193336 |
| Website: |
https://www.sigmaaldrich.cn |
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