Muraglitazar

这是一种PPARα和PPARγ的双重激动剂（EC50值分别为0.32和0.11微米）；对PPARα/γ的选择性高于其他核受体，包括PPARδ、RXRα、RARs、ERα/β、AR和PR；在50微米的浓度下减少油酸处理的HepaRG人肝细胞中脂滴的大小；在db/db小鼠中以10毫克/千克/天的剂量减少血糖、甘油三酯、游离脂肪酸和胰岛素的血浆水平分别为54%、33%、62%和48%；在饮食诱导的肥胖小鼠中以10毫克/千克/天的剂量减少血糖、甘油三酯和胆固醇的血浆水平；在J774小鼠巨噬细胞中抑制LPS诱导的NO产生和IL-6、TNF-α和iNOS蛋白水平的增加；在小鼠中以12.5-50毫克/千克的剂量抑制卡拉胶诱导的足爪水肿。A dual agonist of PPARα and PPARγ (EC50s = 0.32 and 0.11 μM, respectively); selective for PPARα/γ over other nuclear receptors, including PPARδ, RXRα, RARs, ERα/β, AR, and PR; reduces the size of lipid droplets in oleic acid-treated HepaRG human hepatocytes at 50 μM; reduces plasma levels of glucose, triglycerides, free fatty acids, and insulin by 54, 33, 62, and 48%, respectively, in db/db mice at 10 mg/kg per day; reduces plasma levels of glucose, triglycerides, and cholesterol in diet-induced obese mice at 10 mg/kg per day; inhibits LPS-induced increases in NO production and IL-6, TNF-α, and iNOS protein levels in J774 murine macrophages; inhibits carrageenan-induced paw edema in mice at 12.5-50 mg/kg.