6-hydroxy Bexarotene is an oxidative metabolite of bexarotene , a high-affinity ligand for retinoid X receptors (RXRs). 6-hydroxy Bexarotene binds to RXRα, RXRβ, and RXRγ as well as retinoic acid receptor α (RARα; Kds = 3.46, 4.21, 4.83, and 8.17 μM, respectively). It selectively activates RXRα, RXRβ, and RXRγ over RARα, RARβ, and RARγ in vitro (EC50s = 398, 356, 420, 4,414, 2,121, and 2,043 nM, respectively).

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