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.
1.Kick, E., Martin, R., Xie, Y., et al.Liver X receptor (LXR) partial agonists: Biaryl pyrazoles and imidazoles displaying a preference for LXRβBioorg. Med. Chem. Lett.25(2)372-377(2015)