脂蛋白脂肪酶激活剂是一种细胞可渗透的苄基膦酸酯衍生物，可选择性诱导脂蛋白脂肪酶（LPL）mRNA和蛋白水平，但不表现出PPARα或PPARγ激动活性。脂蛋白脂肪酶激活剂可降低动物模型中的血清脂质水平和血浆甘油三酸酯，并伴随高密度脂蛋白胆固醇（HDL-C）升高。脂蛋白脂肪酶激活剂还可以诱导脂肪酸氧化相关的酶，降低游离脂肪酸（FFA），并最大程度地减少脂肪堆积。也有报道抑制血浆中TNF-a和COX-2的水平，并显示出抗肿瘤特性。 Lipoprotein Lipase Activator is a cell-permeable benzylphosphonate derivative that selectively induces lipoprotein lipase (LPL) mRNA and protein levels, but does not exhibit PPARα or PPARγ agonistic activities. Lipoprotein Lipase Activator lowers serum lipid levels and plasma triglycerides with concomitant elevation in high-density lipoprotein cholesterol (HDL-C) in animal models. Lipoprotein Lipase Activator also induces fatty acid oxidation related enzymes, lowers free fatty acids (FFA), and minimizes fat accumulation. Also reported to suppress the plasma levels of TNF-a and COX-2 and displays anti-tumor properties.