GW3965 Hydrochloride, is a potent, selective liver X receptor (LXR) agonist for hLXRα and hLXR. GW3965 has shown potent anti-inflammatory activity in both irritant and allergic contact models of dermatitis, requiring the participation of both LXRα and LXRβ.
GW3965 is a liver X receptor full agonist on hLXRα and hLXRβ. GW3965 has an EC50 = 125 nM in a cell-free ligand-sensing assay of LXRα and profiles as a full agonist on hLXRα and hLXRβ in cell-based assays with EC50 = 190 nM and 30 nM, respectively. It is orally active in mice. When screened against a panel of nuclear receptors, it cross-reacted with only the pregnane X receptor (PXR). The literature agonist, T0901317 (Tularik), had an EC50 = 60 nM and 85 nM in the cell-free and cell-based assays, respectively.
