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| Product Name: | GW 6471 | | Synonyms: | 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;[(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;GW 6471;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]-;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 | | CAS: | 880635-03-0 | | MF: | C35H36F3N3O4 | | MW: | 619.67 | | EINECS: | | Product Categories: | Aromatics;Heterocycles;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals | | Mol File: | Mol File |
| GW 6471 Chemical Properties |
| 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 Codes | Xi | | Risk Statements | 36/37/38 | | Safety Statements | 26-36 | | WGK Germany | 3 |
| GW 6471 Usage And Synthesis |
| 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. | | 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. |
| GW 6471 Preparation Products And Raw materials |
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