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6,2＇,4＇-Trimethoxyflavone

CAS No. : 720675-74-1

MCE 站：6,2＇,4＇-Trimethoxyflavone

产品活性：6,2＇,4＇-Trimethoxyflavone 是一种有效的芳香烃受体 (AHR) 拮抗剂。(AHR) 抑制AHR介导的基因诱导。

研究领域：Immunology/Inflammation

作用靶点：Aryl Hydrocarbon Receptor

In Vitro: 6,2＇,4＇-trimethoxyflavone (TMF) as an AHR ligand that possesses the characteristics of an antagonist having the capacity to compete with agonists, such as 2,3,7,8-tetrachlorodibenzo-p-dioxin ａnd benzo[a]pyrene, thus effectively inhibiting AHR-mediated transactivation of a heterologous reporter ａnd endogenous targets, e.g., CYP1A1, independent of cell lineage or species. Furthermore, TMF displays superior action by virtue of having no partial agonist activity, in contrast to other documented antagonists, e.g., alpha-napthoflavone, which are partial weak agonists. TMF also exhibits no species or promoter dependence with regard to AHR antagonism.
6,2＇,4＇-Trimethoxyflavone (0-100 μM; 72 hours) shows an inhibitory activity of TNF-⍺ production in THP-1 cells, with IC₅₀ of 2.38 μM. 6,2＇,4＇-Trimethoxyflavone shows an inhibitory activity of TNF-α production in B16-F10 cells with IC₅₀ of 1.32 μM.

In Vivo: 6,2＇,4＇-trimethoxyflavone-treated (5 mg/kg/day; i.p.) WT mice shows significantly decreased infarct volume, improved sensorimotor, ａnd nonspatial working memory functions compared with their respective controls.

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