An RXR agonist (EC50s = 28

Bexarotene – 5 mg

Brand:
Cayman
CAS:
153559-49-0
Storage:
-20
UN-No:
Non-Hazardous - /

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.  

 

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SKU: 11571 - 5 mg Category:

Description

An RXR agonist (EC50s = 28, 25, and 20 nM for RXRα, RXRβ, and RXRγ, respectively, in reporter assays); selective for RXRs over RARs (RARs; EC50s = >10 µM for RXRα, RXRβ, and RXRγ); induces apoptosis in MJ, HuT 78, and HH CTCL cells at 10 µM; inhibits lung metastasis and angiogenesis in A549 and MDA-MB-231 mouse xenograft models at 100 mg/kg per day; reduces viral load in the culture supernatant of Vero E6 cells infected with SARS-CoV-2 (EC90 = 9.4 µM) and inhibits SARS-CoV-2 replication in a plaque reduction assay (EC50 = 2.01 µM)

Formal name: 4-[1-(5,6,7,8-tetrahydro-3,5,5,8,8-pentamethyl-2-naphthalenyl)ethenyl]-benzoic acid-d4

Synonyms:  LG 100069|LGD 1069|Ro 26-4455|SR 11247

Molecular weight: 348.5

CAS: 153559-49-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Antivirals||Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Cancer|Angiogenesis||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Endocrinology & Metabolism|Hormones & Receptors|RARs, RORs, & RXRs||Research Area|Immunology & Inflammation|Pulmonary Diseases||Research Area|Infectious Disease|Viral Diseases|Coronaviruses||Research Area|Neuroscience|Neurodegenerative Disorders|Alzheimer’s Disease

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