An RXRα agonist; binds to RXRα (Ki = 12 nM) and induces RXRα-mediated transcription in a mammalian two-hybrid assay (EC50 = 43 nM); an RAR agonist

Fluorobexarotene – 5 mg

Brand:
Cayman
CAS:
1190848-23-7
Storage:
-20
UN-No:
Non-Hazardous - /

Fluorobexarotene is an agonist of retinoid X receptor α (RXRα).{54298} It binds to RXRα (Ki = 12 nM) and induces RXRα-mediated transcription in a mammalian two-hybrid assay (EC50 = 43 nM in Caco-2 cells expressing the human receptor). It also acts as an agonist at the retinoic acid receptor (RAR), inducing 25% of the activity of the RAR agonist all-trans retinoic acid (Item No. 11017) when used at a concentration of 100 nM. Fluorobexarotene (5 and 10 µM) enhances basolateral-to-apical transport of a fluorescent amyloid-β (1-42) (Aβ42) peptide in an in vitro model of blood-brain barrier (BBB) transport when used at concentrations of 5 and 10 µM.{54299} It increases brain-to-peripheral transport of Aβ42 by 3.3-fold in wild-type, but not apolipoprotein E (ApoE) knockout, mice following intraperitoneal administration at a dose of 20 mg/kg.  

 

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Description

An RXRα agonist; binds to RXRα (Ki = 12 nM) and induces RXRα-mediated transcription in a mammalian two-hybrid assay (EC50 = 43 nM); an RAR agonist, inducing 25% of the activity of all-trans retinoic acid at 100 nM; enhances basolateral-to-apical transport of a fluorescent Aβ42 in an in vitro BBB model at 5 and 10 µM; increases brain-to-peripheral transport of Aβ42 by 3.3-fold in wild-type, but not ApoE knockout, mice at 20 mg/kg, i.p.

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

Synonyms: 

Molecular weight: 366.5

CAS: 1190848-23-7

Purity: ≥95%

Formulation: A solid

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