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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.
Keywords:
LG 100069, LGD 1069, Ro 26-4455, SR 11247, 4-[1-(5,6,7,8-tetrahydro-3,5,5,8,8-pentamethyl-2-naphthalenyl)ethenyl]-benzoic acid-d4
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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