GW3965 hydrochloride is a synthetic liver X receptor (LXR) 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. When screened against a panel of nuclear receptors, it cross-reacted with only the pregnane X receptor (PXR).
Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines.
Reciprocal regulation of inflammation and lipid metabolism by liver X receptors.
GW3965, a synthetic liver X receptor (LXR) agonist, reduces angiotensin II-mediated pressor responses in Sprague-Dawley rats.
LXR activation by GW3965 alters fat tissue distribution and adipose tissue inflammation in ob/ob female mice.