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BMS 779788 is a partial agonist of liver X receptor α (LXRα) and LXRβ (Kis = 68 and 14 nM, respectively, in a radioligand binding assay).1 It activates LXRα and LXRβ with EC50 values of 230 and 250 nM, respectively, in a transactivation assay. BMS 779788 increases expression of ATP-binding cassette transporter (ABCA1) in HeLa cells and isolated human and mouse whole blood (EC50s = 33, 1,200, and 120 nM, respectively). It also increases expression of Abca1 and Abcg2 in isolated mouse blood cells but does not increase plasma or hepatic triglycerides when administered at a dose of 10 mg/kg.
WARNING This product is not for human or veterinary use.
1. Liver X receptor (LXR) partial agonists: Biaryl pyrazoles and imidazoles displaying a preference for LXRβ. Bioorg. Med. Chem. Lett. 25(2), 372-377 (2015).