The small molecule PF-429242 was developed as a hypolipidemic agent based on high throughput screening in a Pfizer compound library. PF-429242 is a competitive inhibitor of sterol regulatory element-binding protein (SREBP) site 1 protease (IC50 = 0.175 uM). It is selective for site 1 protease against a panel of serine proteases. PF-429242 inhibits rate of cholesterol synthesis in CHO cells (IC50 = 0.53 uM). PF-429242 inhibits the activity of S1P reversibly and competitively and suppresses the expression level of SREBP target genes, consequently decreasing cellular lipid levels. It has been shown that PF-429242 suppresses hepatic SREBP target genes and inhibits cholesterol and fatty acid synthesis in a mouse model. It also has been reported that PF-429242 suppresses viral replication in cells infected with hepatitis C virus (HCV), Lassa virus, lymphocytic choriomeningitis virus, New World arenaviruses and Dengue virus.

GW0742, also known as GW610742, is a potent and highly selective PPARβ/δ agonist, with IC50 of 1 nM, with 1000-fold selectivity over hPPARα and hPPARγ. GW0742 treatment has a prominent anti-inflammatory effect in 5XFAD mice and suggests that PPARδ agonists may have therapeutic utility in treating AD. GW0742 has the ability to improve glucose homeostasis in diabetic rats through activation of PPAR-δ. Therefore, PPAR-δ is a good target for the development of antidiabetic drugs in the future.

27-Hydroxycholesterol (27-HC) is an endogenous oxysterol produced by the enzyme CYP27A1, with multiple biological functions, including acting as a selective estrogen receptor modulator (SERM) and as an agonist of the liver X receptor (LXR). Because of its estrogenic action, 27-HC stimulates the growth of ER-positive breast cancer cells and has been implicated in limiting the effectiveness of aromatase inhibitors in the treatment of breast cancer.