Bexarotene

Bexarotene

CAT N°: 11571
Price:

From 48.00 40.80

Bexarotene is an agonist of retinoid X receptors (RXRs; EC50s = 28, 25, and 20 nM for RXR?, RXR?, and RXR?, respectively, in reporter assays).{20758} It is selective for RXRs over retinoic acid receptors (RARs; EC50s = >10 µM for RAR?, RAR?, and RAR?). 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-? (1-40) (A?40) and A?42 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.

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 4-[1-(5,6,7,8-tetrahydro-3,5,5,8,8-pentamethyl-2-naphthalenyl)ethenyl]-benzoic acid
  • Correlated keywords
    • ?amyloid LG100069 LGD1069 RO264455 RO26-4455 RO-26-4455 SR11247 targret targretin targretyn targrexin
  • Product Overview:
    Bexarotene is an agonist of retinoid X receptors (RXRs; EC50s = 28, 25, and 20 nM for RXR?, RXR?, and RXR?, respectively, in reporter assays).{20758} It is selective for RXRs over retinoic acid receptors (RARs; EC50s = >10 µM for RAR?, RAR?, and RAR?). 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-? (1-40) (A?40) and A?42 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.

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