T0901317
LXR agonist / Potent high affinity liver X receptor (LXRα and β) agonist, EC50~50 nM.1 Upregulates expression of ABCA1, a reverse cholesterol transporter, resulting in inhibition of cholesterol absorption. Inverse agonist at CAR.2 T0901317 was also shown to be an FXR agonist at lower potency than LXR thus appropriate controls must be employed when using this compound as a pharmacological tool.3 Decreases amyloid beta production in a mouse model of Alzheimer’s disease.4 Inhibits cellular senescence in endothelial cells.5
Biochemicals & reagents
293754-55-9
1 Repa et al. (2000), Regulation of absorption and ABC1-mediated efflux of cholesterol by RXR heterodimers; Science, 289 1524 2 Kanno et al. (2013) T0901317, a potent LXR agonist, is an inverse agonist of CAR; J. Toxicol. Sci., 38 309 3 Houck et al. (2004) T0901317 is a dual LXR/FXR agonist; Mol. Genet. Metab., 83 4079 4 Koldamova et al. (2005) The liver X receptor ligand T0901317 decreases amyloid beta production in vitro and in a mouse model of Alzheimer’s disease; J. Biol. Chem., 280 4079 5 Hayashi et al. (2014) Endothelial cellular senescence is inhibited by liver X receptor activation with an additional mechanism for its atheroprotection in diabetes; Proc. Natl. Acad. Sci. USA, 111 1168
-20°C
TARGET: Transcription factor -- PATHWAY: Cholesterol metabolism; Senescence; Fatty acid metabolism; Cytokine; NFkappaB -- RESEARCH AREA: Oxidative stress; Neuroscience -- DISEASE AREA: Diabetes; AtherosclerosisNeurodegeneration; Obesity; Inflammation