GSK2033

GSK2033 is a LXR antagonist with pIC₅₀s of 7 and 7.4 for LXRα or LXRβ, respectively. IC50 & Target: pIC50: 7 (LXRα), 7.4 (LXRβ)^[1] In Vitro: GSK2033 is a LXR antagonist with pIC₅₀s of 7 and 7.4 for LXRα or LXRβ, respectively. GSK2033 dose-dependently suppresses basal transcription in full-length LXRα or full-length LXRβ cotransfection assays with IC₅₀s of 17 nM and 9 nM, respectively. GSK2033 also effectively suppresses the transcription of an ABCA1 driven luciferase reporter dose-dependently displaying IC₅₀s of 52 nM for LXRα and 10 nM for LXRβ. GSK2033 also suppresses the expression of both of fatty acid synthase (FASN) and SREBP1^[2]. In Vivo: One month treatment of GSK2033 does not have significant effects on hepatic triglyceride levels. Plasma triglyceride levels are also unaffected by treatment with GSK2033^[2].