SGA360 通过一种不需要 AHR 与其同源反应元件（部分拮抗剂）结合的机制，以 AHR 依赖性方式抑制炎症性 SAA1 信号传导。
| Cas No. | 680611-86-3 |
| 化学名 | 3-(2,4-dimethoxyphenyl)-1-(2-propen-1-yl)-7-(trifluoromethyl)-1H-indazole |
| Canonical SMILES | C=CCN1N=C(C2=CC=C(OC)C=C2OC)C3=CC=CC(C(F)(F)F)=C31 |
| 分子式 | C19H17F3N2O2 |
| 分子量 | 362.4 |
| 溶解度 | DMF: 20 mg/ml,DMF:PBS(pH7.2) (1:2): 0.33 mg/ml,DMSO: 10 mg/ml,Ethanol: 2.5 mg/ml |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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. |
