| Size | Price | |
|---|---|---|
| 100mg | ||
| 250mg | ||
| 500mg |
| ln Vitro |
6,2',4'-Trimethoxyflavone (TMF), as an AHR ligand, possesses antagonist qualities and is able to outcompete agonists like benzo[a]pyrene and 2,3,7,8-tetrachlorodibenzo-p-dioxin. This effectively prevents AHR-mediated transactivation of endogenous targets (like CYP1A1) and heterologous reporters, irrespective of kind of cell. TMF also works very well because it is not a partial agonist, unlike other known antagonists like α-naphthoflavone, which is a mild partial agonist. In AHR antagonistic interactions, TMF likewise exhibits no promoter or species dependence [1]. IC50 of 2.38 μM was observed for 6,2',4'-Trimethoxyflavone (0-100 μM; 72 hours) on TNF-⍺ production in THP-1 cells. The generation of TNF-α in B16-F10 cells is inhibited by 6,2',4'-trimethoxyflavone, with an IC50 of 1.32 μM.
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|---|---|
| ln Vivo |
Compared with respective controls, WT mice treated with 6,2',4'-trimethoxyflavone (5 mg/kg/day; i.p.) demonstrated substantial decreases in infarct volume, sensorimotor and non-spatial skills. Memory function is improved[3].
|
| Cell Assay |
Cell viability assay [2]
Cell Types: THP-1 cells, B16-F10 cells Tested Concentrations: 0-100 μM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibitory activity on TNF-⍺ production in THP-1 cells and B16-F10 cells . |
| Animal Protocol |
Animal/Disease Models: Male C57BL/6 wild-type (WT) mice, AHRcKO mice [3]
Doses: 5 mg/kg/day Route of Administration: intraperitoneal (ip) injection Experimental Results: Both TMF-treated mice and AHRcKO mice can reduce acute cerebral infarction Infarction and dysfunction. |
| References |
[1]. Murray IA, et al. Antagonism of aryl hydrocarbon receptor signaling by 6,2',4'-trimethoxyflavone [published correction appears in J Pharmacol Exp Ther. 2018 Nov;367(2):291]. J Pharmacol Exp Ther. 2010;332(1):135-144.
[2]. Apaza T L, et al. Flavonoids of Tripodanthus acutifolius inhibit TNF-α production in LPS-activated THP-1 and B16-F10 cells. J Ethnopharmacol. 2019;242:112036. [3]. Chen WC, et al. Aryl hydrocarbon receptor modulates stroke-induced astrogliosis and neurogenesis in the adult mouse brain. J Neuroinflammation. 2019;16(1):187. Published 2019 Oct 12. |
| Molecular Formula |
C18H16O5
|
|---|---|
| Molecular Weight |
312.317
|
| CAS # |
720675-74-1
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| SMILES |
COC1=CC=C(C2=CC(=O)C3=CC(=CC=C3O2)OC)C(OC)=C1
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~5 mg/mL (~16.01 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.5 mg/mL (1.60 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.5 mg/mL (1.60 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2018 mL | 16.0092 mL | 32.0184 mL | |
| 5 mM | 0.6404 mL | 3.2018 mL | 6.4037 mL | |
| 10 mM | 0.3202 mL | 1.6009 mL | 3.2018 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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