T0901317 is a potent and selective agonist for both LXR and FXR, with EC50 of ~50 nM and 5 μM, respectively.

The Liver X Receptors (LXRα and LXRβ) are nuclear hormone receptors whose native ligands are oxysterols, such as 22(R)-hydroxycholesterol. The LXRs regulate the oxysterol-induced expression of cholesterol 7α-hydroxylase, the rate limiting enzyme of classic bile acid synthesis. T0901317 is a potent and selective agonist for both LXRα and LXRβ, with an EC50 of about 50 nM.T0901317 acting through LXR and in concert with its RXR heterodimerization partner induces the expression of the ABCA1 reverse cholesterol transporter. This acts to increase the efflux of cholesterol from enterocytes and thus inhibit the overall absorption of cholesterol.