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PPARβ/δ inverse agonist
DG-172 是一种口服活性强的 PPARβ/δ 逆激动剂(IC50 = 26.9 nM)。DG-172 在体外抑制小鼠肌母细胞中的 Angptl4 基因表达(IC50 = 9.5 nM)。 -
peptidoleukotrienes antagonist
RG-12525 is a specific, competitive and orally effective antagonist of the peptidoleukotrienes, LTC4, LTD4 and LTE4, inhibiting LTC4-, LTD4- and LTE4-induced guinea pig parenchymal strips contractions, with IC50s of 2.6 nM, 2.5 nM and 7 nM, respectively. RG-12525 is also a peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonist with an IC50 of approximately 60 nM and a potent inhibitor of CYP3A4, with a Ki value of 0.5 µM.