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GW3965 HCl is a selective, orally active non-steroidal agonist for the liver X receptor (LXR) [1].

Nuclear receptors LXRα  and LXRβ have an important role in control of cholesterol and fatty acid metabolism in multiple cell types. Activation of these receptors promotes bile acid synthesis in liver, inhibits intestinal cholesterol absorption and stimulates cholesterol efflux in macrophages, which will then reduce atherosclerotic risk [2].

In a cell-free ligand-sensing assay, GW3965 recruits the steroid receptor coactivator 1 to human LXRR with an EC50 of 125 nM. In cell-based reporter gene assays, GW3965 plays as a full agonist on hLXRα and hLXRβ with EC50 of 190 and 30 nM, respectively [1].

Treatment C57BL/6 mice with 10 mg/kg GW3965 HCl orally, GW3965 HCl increased the plasma concentrations of HDL cholesterol by 30% and enhanced the expression of the reverse cholesterol transporter ABCA1 in the small intestine and peripheral macrophages [1]. In male Sprague–Dawley rats, GW3965 decreased Ang II-mediated vasopressor responses and reduced ATR gene expression, which suggested GW3965 can affect vascular reactivity [3].

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