LY518674 是高效、选择性的 PPARα 拮抗剂，对人 human PPARα 作用的 EC50 值为 42 nM。LY518674 能降低甘油三酸酯，增加 HDL-C，可用于治疗动脉粥样硬化。
LY518674 is a potent, selective PPARα antagonist, with an EC50 of 42 nM for human PPARα. LY518674 reduces triglycerides in and increased HDL-C and is used for the treatment of atherosclerosis[1][2][3].
[1]. Bravo Y, et al. Identification of the first potent, selective and bioavailable PPARα antagonist. Bioorg Med Chem Lett. 2014 May 15;24(10):2267-72. [2]. Nissen SE, et al. Effects of a potent and selective PPAR-alpha agonist in patients with atherogenic dyslipidemia or hypercholesterolemia: two randomized controlled trials. JAMA. 2007 Mar 28;297(12):1362-73. [3]. Khera AV, et al. Potent peroxisome proliferator-activated receptor-α agonist treatment increases cholesterol efflux capacity in humans with the metabolic syndrome. Eur Heart J. 2015 Nov 14;36(43):3020-2.
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