T0901317

T0901317 is an orally active and highly selective LXR agonist with an EC₅₀ of 20 nM for LXRα^[1]. T0901317 activates FXR with an EC₅₀ of 5 μM^[2]. T0901317 is RORα and RORγ dual inverse agonist with K_i values of 132 nM and 51 nM, respectively^[3]. T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice^[4][5]. IC50 & Target: EC50: 20 nM (LXRα) and 5 μM (FXR)^[1][2]
Ki: 132 nM (RORα) and 51 nM (RORγ)^[3] In Vitro: T0901317 (5-50 μM; 72 hours) significantly inhibits cellular proliferation in CaOV3, SKOV3, A2780 (human ovarian carcinoma cell lines) in a dose-dependent and time-dependent manner^[5].
T0901317 (10 μM; 24-72 hours) decreases the percentage of cells in S phase and increases the percentage of cells in the G0/G1 phase, indicating a cell cycle arrest at the G1-S checkpoint. The percentage of cells in G0/G1 phase increases in a time-dependent manner^[5].
T0901317 (10-40 μM; 24 hours ) results in a significant increase of cells in early apoptosis^[5].
T0901317 (5-40 μM; 48 hours) results in an increase of p21 and p27 protein expression in a dose-dependent manner after 48 hours^[5].
In Vivo: T0901317 (10 mg/kg/day; orally; for 12 weeks) inhibits the progression of atherosclerosis^[5].
T0901317 (i.p.; 50 mg/kg; twice weekly for 7 days) can protect male C57BL/6 mice from high fat diet-induced obesity and insulin resistance^[6].