CAS No.: 317318-84-6
Other Name: GW0742;[4-[[[2-[3-FLUORO-4-(TRIFLUOROMETHYL)PHENYL]-4-METHYL-5-THIAZOLYL]METHYL]THIO]-2-METHYLPHENOXY]ACETIC ACID;4-[2-(3-FLUORO-4-TRIFLUOROMETHYL-PHENYL)-4-METHYL-THIAZOL-5-YLMETHYLSULFANYL]-2-METHYL-PHENOXY-ACETIC ACID;4-[[[2-[3-Fluoro-4-(trifluoromethyl)phenyl]-4-methyl-5-thiazolyl]methyl]thio]-2-methylphenoxy]AceticAcid;4-[2-(3-Fluoro-4-trifluoromethyl-phenyl)-4-methyl-thiazol-5-ylmethylsulfanyl]- 2-methyl-phenoxy}-acetic acid;Acetic acid, 2-[4-[[[2-[3-fluoro-4-(trifluoroMethyl)phenyl]-4-Methyl-5-thiazolyl]Methyl]thio]-2-Methylphenoxy]-;2-(4-(((2-(3-Fluoro-4-(trifluoromethyl)phenyl)-4-methylthiazol-5-yl)methyl)thio)-2-methylphenoxy);GW 0742X
Boiling Point: 591.476ºC at 760 mmHg
Flash point: 311.514ºC
Storage temp.: -20ºC
A small molecule agonist of the human Peroxisome Proliferator-Activated Recept δ (PPAR δ). It shows an EC50 of 1.1 nM against PPAR δ with 100-fold selectivity over the other human subtypes.
GW0742 is a selective PPARδ agonist (EC50 = 1.1 nM) that exhibits 1,000-fold selectivity over the other human PPAR subtypes. GW 0742 exhibits time-dependent neuroprotection in low KCl-induced apoptosis in cerebellar granule neuronal cultures. Despite the neuroprotective properties observed, prolonged (48h) incubation with GW 0742 produced significant inherent toxicity. This cell death was determined to be apoptotic as identified with the TUNEL assay. The transcription factor peroxisome proliferator-activated receptor δ (PPARδ) is a member of the superfamily of nuclear hormone receptors and is implicated both in lipid metabolism and in the regulation of genes with potential roles in neurotoxicity. GW 0742 is a selective PPARδ agonist (EC50 = 1.1 nM) that exhibits 1,000-fold selectivity over the other human PPAR subtypes. GW 0742 exhibits time-dependent neuroprotection in low KCl-induced apoptosis in cerebellar granule neuronal cultures. Despite the neuroprotective properties observed, prolonged (48h) incubation with GW 0742 produced significant inherent toxicity. This cell death was determined to be apoptotic as identified with the TUNEL assay.
GW0742 (GW610742) is a potent and highly selective PPARδ agonist. EC50 values are 1nM, 1.1μM and 2 μM for transactivation of human PPARδ, -α, and -γ receptors respectively. IC50 value: 1nM, 1.1μM and 2 μM (EC50, for PPARδ, -α, and -γ) Target: PPAR in vivo: GW0742 is a synthetic high affinity PPAR β/δ agonist, and its possible role in preventing the advance of inflammatory and apoptotic processes induced by bleomycin, that long-term leads to the appearance of pulmonary fibrosis. Our data showed that GW0742-treatment (0.3 mg/Kg, 10 percent DMSO, i.p.) has therapeutic effects on pulmonary damage, decreasing many inflammatory and apoptotic parameters detected by measurement of: 1) cytokine production; 2) leukocyte accumulation, indirectly measured as decrease of myeloperoxidase (MPO) activity; 3) IkBα degradation and NF-kB nuclear translocation; 4) ERK phosphorylation; 5) stress oxidative by NO formation due to iNOS expression; 6) nitrotyrosine and PAR localization; 7) the degree of apoptosis, evaluated by Bax and Bcl-2 balance, FAS ligand expression and TUNEL staining. Taken together, our results clearly show that GW0742 reduces the lung injury and inflammation due to the intratracheal BLEO--instillation in mice.
|S4 (Andarine, GTX-007)