1. Immunology/Inflammation
  2. Aryl Hydrocarbon Receptor
  3. 6,2',4'-Trimethoxyflavone

6,2',4'-Trimethoxyflavone 

Cat. No.: HY-103220
Handling Instructions

6,2',4'-Trimethoxyflavone is a potent aryl hydrocarbon receptor (AHR) antagonist. 6,2',4'-Trimethoxyflavone represses AHR-mediated gene induction.

For research use only. We do not sell to patients.

6,2',4'-Trimethoxyflavone Chemical Structure

6,2',4'-Trimethoxyflavone Chemical Structure

CAS No. : 720675-74-1

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Description

6,2',4'-Trimethoxyflavone is a potent aryl hydrocarbon receptor (AHR) antagonist. 6,2',4'-Trimethoxyflavone represses AHR-mediated gene induction[1].

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[1].
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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: THP-1 cells, B16-F10 cells
Concentration: 0-100 μM
Incubation Time: 72 hours
Result: Showed inhibitory activity of TNF-⍺ production in THP-1 cells and B16-F10 cells.
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[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57BL/6 wild-type (WT) mice, AHRcKO mice[3]
Dosage: 5 mg/kg/day
Administration: I.p.
Result: Both TMF-treated and AHRcKO mice attenuated acute cerebral infarction and functional impairments.
Molecular Weight

312.32

Formula

C₁₈H₁₆O₅

CAS No.
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Product Name:
6,2',4'-Trimethoxyflavone
Cat. No.:
HY-103220
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