Hangzhou Fuluo Biological Technology Co.,Ltd.

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Other name:GW610742




Appearance:white powder


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. 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.