A selective modulator of AhR; competitively binds AhR (IC50 = 3 µM); represses IL-1β-induced SAA1 gene expression in Huh7 cells; reduces inflammation and decreases the mRNA expression of COX-2

SGA360 – 1 mg

Brand:
Cayman
CAS:
680611-86-3
Storage:
-20
UN-No:
Non-Hazardous - /

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.{38254,12907} SGA360 competitively binds to AhR (IC50 = 3 µM) and represses serum amyloid A 1 (SAA1) gene expression induced by IL-1β in Huh7 cells.{38254} 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.{38253}  

 

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Description

A selective modulator of AhR; competitively binds AhR (IC50 = 3 µM); represses IL-1β-induced SAA1 gene expression in Huh7 cells; reduces inflammation and decreases the mRNA expression of 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; reduces acute inflammation in murine models of septic shock, gout, and peritonitis when the high-affinity AhR variant is expressed,

Formal name: 3-(2,4-dimethoxyphenyl)-1-(2-propen-1-yl)-7-(trifluoromethyl)-1H-indazole

Synonyms: 

Molecular weight: 362.4

CAS: 680611-86-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Allosteric Modulators||Research Area|Immunology & Inflammation|Arthritis (Non-autoimmune)||Research Area|Immunology & Inflammation|Innate Immunity|Sepsis/Shock

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