T0901317 | LXR Agonist

T0901317 (293754-55-9) is a  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

References/Citations:

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