SGA360

SGA360 is a selective modulator of the aryl hydrocarbon receptor (AhR), which is a ligand-dependent transcription factor that mediates the toxicity of certain xenobiotics and polyaromatic hydrocarbons. SGA360 competitively binds to AhR (IC50 = 3 uM) and represses serum amyloid A 1 (SAA1) gene expression induced by IL-1β in Huh7 cells. It also reduces inflammation and decreases the mRNA expression of the inflammatory mediators COX-2, IL-6, IL-1β, SAA3, and IL-10 in wild-type, but not AhR knockout, mice in a model of inflammatory ear edema. SGA360 also reduces acute inflammation in murine models of septic shock, gout, and peritonitis when the high-affinity AhR variant is expressed.