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LXRβ agonist-2 是一种高效 β 选择性肝 X 受体 (LXRβ) 激动剂,EC50为 7 nM,其选择性是 LXRα (EC50=200 nM) 的 28.5 倍,用于治疗动脉粥样硬化。
LXRβ agonist-2 is a highly potent and β-selective liver X receptor (LXRβ) agonist with EC50 of 7 nM, displays 28.5-fold selectivity over LXRα (EC50=200 nM) and used in the treatment of atherosclerosis[1]. EC50: 7 nM (LXRβ), 200 nM (LXRα)[1]
[1]. Koura M,et al. Discovery of a 2-hydroxyacetophenone derivative as an outstanding linker to enhance potency and β-selectivity of liver X receptor agonist. Bioorg Med Chem. 2016 Aug 15;24(16):3436-46.
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