Bexarotene
Bexarotene is a retinoid compound that binds and activates retinoid X receptors (RXRs) and is approved to treat cutaneous T cell lymphoma. Bexarotene displays a wide variety of beneficial activities, such as anticancer chemotherapeutic, anti-hyperlipidemic, and neuroprotective properties. Bexarotene has shown pre-clinical and clinical efficacy in treatment of other cancers, increasing apoptosis and inducing tumor regression in vitro and in vivo. Bexarotene’s activation of RXRs also results in activation of PPARα signaling, decreasing triglyceride levels and increasing HDL cholesterol levels in vivo. This compound interacts with nuclear hormone receptor Nurr1-RXR heterodimers, reversing behavioral deficits induced by 6-OH DA in rat models of Parkinson’s disease. Additionally, bexarotene activation of RXRs induces ApoE-dependent clearance of amyloid-β (Aβ) peptides and plaques, reversing cognitive deficits in animal models of Alzheimer’s disease.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18843751
| Cas No. |
153559-49-0 |
|---|---|
| Purity |
≥98% |
| Formula |
C24H28O2 |
| Formula Wt. |
348.48 |
| IUPAC Name |
4-[1-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)ethenyl]benzoicacid |
| Synonym |
Targretin, Targretyn, LGD-1069 |
| Solubility |
Practically insoluble in water. Soluble in DMSO (≥60 mg/ml). |
| Appearance |
White to off white powder |
McFarland K, Spalding TA, Hubbard D, et al. Low Dose Bexarotene Treatment Rescues Dopamine Neurons and Restores Behavioral Function in Models of Parkinsons Disease. ACS Chem Neurosci. 2013 Oct 11. [Epub ahead of print]. PMID: 24117438.
Schadt CR. Topical and oral bexarotene. Dermatol Ther. 2013 Sep;26(5):400-3. PMID: 24099070.
Aicardi G. New Hope from an Old Drug: Fighting Alzheimers Disease with the Cancer Drug Bexarotene (Targretin)? Rejuvenation Res. 2013 Sep 19. [Epub ahead of print]. PMID: 24047423.
Quéreux G, Saint-Jean M, Peuvrel L, et al. Bexarotene in cutaneous T-cell lymphoma: third retrospective study of long-term cohort and review of the literature. Expert Opin Pharmacother. 2013 Sep;14(13):1711-21. 10. PMID: 23837676.
Mukherjee R, Strasser J, Jow L, et al. RXR agonists activate PPARalpha-inducible genes, lower triglycerides, and raise HDL levels in vivo. Arterioscler Thromb Vasc Biol. 1998 Feb;18(2):272-6. PMID: 9484993.
