Biochem/physiol Actions

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.

Features and Benefits

This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

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Packaging

5, 25 mg in glass bottle