A high affinity synthetic ligand for both RORα and RORγt acting as an inverse agonist. It binds specifically to the ligand-binding domain, inducing a conformational change which leads to diminished affinity for co-activators and increased affinity for co-repressors resulting in suppression of...
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A high affinity synthetic ligand for both RORα and RORγt acting as an inverse agonist. It binds specifically to the ligand-binding domain, inducing a conformational change which leads to diminished affinity for co-activators and increased affinity for co-repressors resulting in suppression of transcriptional activity. It inhibits the development of murine TH17 cells and suppresses the expression of cytokines. Suppresses insulitis and prevents hyperglycemia in a type 1 diabetes mouse model. Protects against pathologic neovascularization in various mouse models of retinopathy. Active in vivo
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