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Author Topic:   GW3965
AdaBrown
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posted 11-21-2016 05:27 AM     Click Here to See the Profile for AdaBrown   Click Here to Email AdaBrown     Edit/Delete Message Reply w/Quote
GW3965 is a potent, selective LXR agonist for hLXRα and hLXRβ. When screened against a panel of nuclear receptors, it cross-reacted with only the pregnane X receptor (PXR). In Vitro: Recruit the steroid receptor coactivator 1 to human LXRα with EC50 of 125 nM in a cell-free ligand-sensing assay; Potent antagonistic activity against hLXRα and hLXRβ in cell-based assays with EC50 of 190 nM and 30 nM, respectively; In human islets, GW3965 (1 μM) reduces expression of selected pro-inflammatory cytokines including IL-8, monocyte chemotactic protein-1 and tissue factor In Vivo: At a dose of 10 mg/kg upregulates ABCA1 expression 8-fold and raises circulating levels of HDL by 30% with Cmax of 12.7 μg/mL and t1/2 of 2 hours.

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