GW 6471
Uses In vitro Targets- Product Name
- GW 6471
- CAS No.
- 880635-03-0
- Chemical Name
- GW 6471
- Synonyms
- GW 6471;GW 6471 USP/EP/BP;(S,Z)-N-(3-(4-(2-(5-Methyl-2-phenyloxazol-4-yl)ethoxy)phenyl)-2-((4-oxo-4-(4-(trifluoromethyl)phenyl)but-2-en-2-yl)amino)propyl)propionamide;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
- CBNumber
- CB4207232
- Molecular Formula
- C35H36F3N3O4
- Formula Weight
- 619.67
- MOL File
- Mol file
GW 6471 Property
- 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 and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- G5045
- Product name
- GW6471
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $281
- Updated
- 2024/03/01
- Product number
- 11697
- Product name
- GW 6471
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $44
- Updated
- 2024/03/01
- Product number
- 11697
- Product name
- GW 6471
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $151
- Updated
- 2024/03/01
- Product number
- 11697
- Product name
- GW 6471
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $235
- Updated
- 2024/03/01
- Product number
- 11697
- Product name
- GW 6471
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $533
- Updated
- 2024/03/01
GW 6471 Chemical Properties,Usage,Production
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
Uses
GW 6471 is a peroxisome proliferator-activated receptor α (PPARα) antagonist. GW 6471 has been shown to enhance the binding affinity of the PPARα ligand-binding domain to the co-repressor proteins SMRT and NCoR.
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