CAS: 368451-07-4

6-Hydroxy Bexarotene, an oxidative metabolite of bexarotene, serves as a high-affinity ligand for retinoid X receptors (RXRs), specifically binding to RXRα, RXRβ, and RXRγ, as well as to the retinoic acid receptor α (RARα) with dissociation constants (Kds) of 3.46, 4.21, 4.83, and 8.17 μM, respectively. It demonstrates selective activation of RXRα, RXRβ, and RXRγ over RARα, RARβ, and RARγ in vitro, with half-maximal effective concentrations (EC50s) of 398, 356, 420, 4,414, 2,121, and 2,043 nM, respectively.

Stability Light Sensitive Applications A metabolite of Bexarotene (B336750). References Hashimoto, S., et al.: Xenobiotica, 24, 1177 ( 1994), Boehm, M., et al.: J. Med. Chem., 38, 3146 (1995), Shirley, M.A., et al.: Drug Metab. Dispos., 25, 1144 (1997),

6-Hydroxy bexarotene is a synthetic retinoid that binds to the retinoic acid receptors in the nucleus and activates gene expression. It is used for the treatment of t-cell lymphoma and cutaneous T-cell lymphoma. 6-Hydroxy bexarotene is metabolized by human liver enzymes, which leads to minimal systemic exposure. The drug has been shown to have transactivating activity in vitro as well as in humans. This activity has been shown to be higher in untreated patients than in those who are on immunosuppressive therapy or other treatments.