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编 号:F436969
分子式:C18H16O5
分子量:312.32
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5mg
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10mg
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25mg
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50mg
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100mg
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生物活性:
6,2',4'-Trimethoxyflavone is a potent aryl hydrocarbon receptor (AHR) antagonist. 6,2',4'-Trimethoxyflavone represses AHR-mediated gene induction.

体内研究:
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.Animal Model:Male C57BL/6 wild-type (WT) mice, AHRcKO mice
Dosage:5 mg/kg/day
Administration:I.p.
Result:Both TMF-treated and AHRcKO mice attenuated acute cerebral infarction and functional impairments.

体外研究:
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 IC50of 1.32 μM.
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