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.^1,2 SGA360 competitively binds to AhR (IC₅₀ = 3 µM) and represses serum amyloid A 1 (SAA1) gene expression induced by IL-1β in Huh7 cells.¹ 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.³

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1. Murray, I.A., Krishnegowda, G., DiNatale, B.C., et al. Development of a selective modulator of aryl hydrocarbon (Ah) receptor activity that exhibits anti-inflammatory properties. Chem. Res. Toxicol. 23(5), 955-966 (2010).

2. Denison, M.S., and Nagy, S.R. Activation of the aryl hydrocarbon receptor by structurally diverse exogenous and endogenous chemicals. Annu. Rev. Pharmacol. Toxicol. 43, 309-334 (2003).

3. Muku, G.E., Lahoti, T.S., Murray, I.A., et al. Ligand-mediated cytoplasmic retention of the Ah receptor inhibits macrophage-mediated acute inflammatory responses. Lab Invest. (2017).