产品描述:
Bexarotene is an agonist of retinoid X receptors (RXRs; EC50s = 28, 25, and 20 nM for RXRα, RXRβ, and RXRγ, respectively, in reporter assays).{20758} It is selective for RXRs over retinoic acid receptors (RARs; EC50s = >10 µM for RARα, RARβ, and RARγ). Bexarotene (10 µM) induces apoptosis in MJ, HuT 78, and HH cutaneous T cell lymphoma (CTCL) cells, as well as inhibits lung metastasis and angiogenesis in A549 and MDA-MB-231 mouse xenograft models when administered at a dose of 100 mg/kg per day.{58126,58127} It reduces increased brain interstitial fluid levels of amyloid-β (1-40) (Aβ40) and Aβ42 in the APP/PS1 transgenic mouse model of Alzheimer’s disease.{20759} It also reduces viral load in the culture supernatant of Vero E6 cells infected with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2; EC90 = 9.4 µM) and inhibits SARS-CoV-2 replication in a plaque reduction assay (EC50 = 2.01 µM).{59330} Formulations containing bexarotene have been used in the treatment of CTCL.