Drug intelligence / Profile preview

GW3965

Development stage
Preclinical
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

GW3965 is a selective, orally active, non-steroidal small molecule agonist of the liver X receptor (LXR), acting as a full agonist at both LXRα and LXRβ with EC50 values of approximately 190 nM and 30 nM, respectively. It upregulates ABCA1 gene expression and increases circulating HDL levels. In preclinical models, it demonstrates antiatherogenic activity by reducing angiotensin II-mediated blood pressure increases and modulating vascular reactivity. The compound is primarily used in research settings to study lipid metabolism, cardiovascular disease mechanisms, and neuroprotection following brain injury.

Other names
3-(3-(N-(2-Chloro-3-trifluoromethylbenzyl)(2,2-diphenylethyl)amino)propoxy)phenylacetic acid
02

Targets

LXRB (Liver X receptor beta)NR1H3 (Liver X receptor beta)

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