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6,2',4'-Trimethoxyflavone
芳基烃受体拮抗剂
目录号: PC14883 纯度: ≥98%
CAS No. :720675-74-1
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中文名称
6,2',4'-Trimethoxyflavone
中文别名
2-(2,4-二甲氧基苯基)-6-甲氧基-4H-色烯-4-酮
英文名称
6,2',4'-Trimethoxyflavone
英文别名
6,2',4'-Trimethoxyflavone;2-(2,4-dimethoxyphenyl)-6-methoxy-4H-chromen-4-one;-Trimethoxyflavone
Cas No.
720675-74-1
分子式
C18O5H16
分子量
312.32
包装储存
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
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.

性状

Solid

体外研究(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.

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

Cell Viability Assay

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.
体内研究(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.

Medlife 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
Dosage: 5 mg/kg/day
Administration: I.p.
Result: Both TMF-treated and AHRcKO mice attenuated acute cerebral infarction and functional impairments.
运输条件

Room temperature or refrigerated transportation.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献
溶解度数据
体外研究: 

DMSO : 5 mg/mL (16.01 mM; Need ultrasonic)

配制储备溶液
浓度 溶剂体积 质量 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
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    建议依照次序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 0.5 mg/mL (1.60 mM); Clear solution

    此方案可获得 ≥ 0.5 mg/mL (1.60 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH?O 中,得到澄清透明的生理盐水溶液
  • 2.

    建议依照次序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 0.5 mg/mL (1.60 mM); Clear solution

    此方案可获得 ≥ 0.5 mg/mL (1.60 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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