5-Methoxyflavone

天然产物 黄酮类 Flavonoids

5-Methoxyflavone  纯度: 99.71%

5-Methoxyflavone,是一种类黄酮,是DNA聚合酶 β (DNA polymerase-beta) 的抑制剂和 β-淀粉样蛋白毒性的神经保护剂。拥有中枢神经系统镇静剂的作用,通过调控嗜离子 GABAA 受体来实现。

5-Methoxyflavone

5-Methoxyflavone Chemical Structure

CAS No. : 42079-78-7

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥550 In-stock
25 mg ¥500 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

5-Methoxyflavone 相关产品

相关化合物库:

  • Natural Product Like Compound Library
  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Anti-Aging Compound Library
  • Neuroprotective Compound Library

生物活性

5-Methoxyflavone, belonged to Flavonoid family, is a DNA polymerase-beta inhibitor and neuroprotective agent against beta-amyloid toxicity. possess central nervous system (CNS) depressant effect mediated through the ionotropic GABAA receptors.

IC50 & Target

DNA polymerase-beta[1].

体外研究
(In Vitro)

5-Methoxyflavone (compound 1) is identified as a candidate compound endowed with the ability to inhibit DNA pol-β in multiple and to prevent cell-cycle initiation and subsequent neuronal apoptosis in Aβ-challenged primary neuronal cultures. 5-methoxyflavone (10-30 μM) is able to significantly enhance toxicity of MMS on 92TAg cells. 5-Methoxyflavone (1 or 10 μM) significantly reduces polymerase activity on a gapped substrate[1].
5-Methoxyflavone (5-MF, 0-100 μg/mL) results in a time dependent reduction in the levels of antiapoptotic proteins cFLIP, Mcl-1 and an increase in the proapoptotic protein BAX. 5-MF induces both TRAIL-R1(DR4) and TRAIL-R2 (DR5) in a time-dependent manner[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

5-Methoxyflavone (100, 150 mg/kg, i.p) significantly decreases the latency time to loss of righting reflex. 5-Methoxyflavone (50, 100 and 150 mg/kg, i.p) exhibits a significant and dose-dependent reduction in the spontaneous locomotor activity. 5-Methoxyflavone (50, 100 mg/kg, i.p) reduces the rearing response. 5-Methoxyflavone (100, 125 and 150 mg/kg, i.p) completely abolishesed the grooming response similar to diazepam treated animals[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

252.26

Formula

C16H12O3

CAS 号

42079-78-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 125 mg/mL (495.52 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.9642 mL 19.8208 mL 39.6416 mL
5 mM 0.7928 mL 3.9642 mL 7.9283 mL
10 mM 0.3964 mL 1.9821 mL 3.9642 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,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,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (8.25 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (8.25 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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 ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (8.25 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (8.25 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (8.25 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (8.25 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
  • [1]. Merlo S, et al. Identification of 5-Methoxyflavone as a Novel DNA Polymerase-Beta Inhibitor and Neuroprotective Agent against Beta-Amyloid Toxicity. J Nat Prod. 2015 Nov 25;78(11):2704-11.

    [2]. Shanmugasundaram J, et al. Sedative-hypnotic like effect of 5-methoxyflavone in mice and investigation on possible mechanisms by in vivo and in silico methods. Biomed Pharmacother. 2018 Dec;108:85-94.

    [3]. Wudtiwai B, et al. Methoxyflavone derivatives modulate the effect of TRAIL-induced apoptosis in human leukemic cell lines. J Hematol Oncol. 2011 Dec 21;4:52.