gw-3965

GW3965 hydrochloride (GW3965 HCl) belongs to synthetic small molecules and is a liver X receptor (LXR) agonist (hLXRα EC50 = 190 nM; hLXRβ EC50 = 30 nM) with subtype selectivity, cell permeability, and oral activity. This compound is used in research related to metabolism, inflammation, and neuropathic pain.

GW3965 is a potent and selective agonist of liver X receptor (LXR) with EC50 values of 190 nM for hLXRα and 30 nM for hLXRβ [1] [2] [3].

FITC-GW3965, a fluorescence-labeled liver X receptor β (LXRβ) agonist, is derived from GW3965 by substituting its trifluoromethyl group with an amide linkage to FITC. This tracer facilitates the study of LXRβ function [1].

22(S)-hydroxy Cholesterol is a synthetic oxysterol and a modulator of the liver X receptor (LXR). [1] t prevents monocyte chemoattractant protein 1 (MCP-1) expression induced by the LXR agonist GW 3965 in primary hepatocytes and downregulates mRNA expression of the LXR target genes CD36, ACSL1, and SCD-1 in human myotubes. It decreases triacylglycerol and diacylglycerol synthesis from labeled palmitate and acetate, respectively, in human myoblasts by 50% when used at a concentration of 10 uM. 22(S)-hydroxy Cholesterol also reduces fatty acid synthase (FAS) reporter activity through an LXR response element in the promoter region in COS-1 cells transfected with RXRα and LXRα and decreases the expression of MCP-1 and CCR2 in a mouse model of chronic ethanol consumption.[1] [2] Dietary supplementation of 22(S)-hydroxy cholesterol (30 mg/kg per day) leads to less body weight gain and lower liver triacylglycerol levels in rats when fed either a regular chow or high-fat diet as well as prevents an increase in plasma triacylglycerol levels resulting from a high-fat diet.[3]