Bexarotene

Bexarotene is an agonist of retinoid X receptors (RXRs, EC50s = 28, 25, and 20 nM for RXRalpha, RXRbeta, and RXRgamma, respectively, in reporter assays). It is selective for RXRs over retinoic acid receptors (RARs, EC50s = >10 µM for RARalpha, RARbeta, and RARgamma). 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. It reduces increased brain interstitial fluid levels of amyloid-beta (1-40) (Abeta40) and Abeta42 in the APP/PS1 transgenic mouse model of Alzheimer's disease. 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). Formulations containing bexarotene have been used in the treatment of CTCL.Formal Name: 4-[1-(5,6,7,8-tetrahydro-3,5,5,8,8-pentamethyl-2-naphthalenyl)ethenyl]-benzoic acid. CAS Number: 153559-49-0. Synonyms: LG 100069, LGD 1069, Ro 26-4455, SR 11247. Molecular Formula: C24H28O2. Formula Weight: 348.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMF:PBS (pH 7.2)(1:3): 0.25 mg/ml, DMSO: 10 mg/ml, Ethanol: 0.5 mg/ml. lambdamax: 256 nm. SMILES: CC1(C)C2=C(C=C(C)C(/C(C3=CC=C(C(O)=O)C=C3)=C([H])/[H])=C2)C(C)(C)CC1. InChi Code: InChI=1S/C24H28O2/c1-15-13-20-21(24(5,6)12-11-23(20,3)4)14-19(15)16(2)17-7-9-18(10-8-17)22(25)26/h7-10,13-14H,2,11-12H2,1,3-6H3,(H,25,26). InChi Key: NAVMQTYZDKMPEU-UHFFFAOYSA-N.