纯度:98% by TLC,;NMR (Conforms)
分子式:C15H13F6N6O4S2
分子量:477.39
溶剂:DMSO (40 mg/ml) Ethanol (40 mg/ml)
性状:Cream-colored solid
存储:-20°C
Activity (short version):RORag inverse agonist
Function / Pharmacology: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 activity1. It inhibits the development of murine TH17 cells2 and suppresses the expression of cytokines1. Suppresses insulitis and prevents hyperglycemia in a type 1 diabetes mouse model3. Protects against pathologic neovascularization in various mouse models of retinopathy4. Active in vivo