4′-Hydroxychalcone(Synonyms: 4′-羟基查耳酮)

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4′-Hydroxychalcone (Synonyms: 4′-羟基查耳酮) 纯度: ≥98.0%

4′-Hydroxychalcone 是从甘草根中分离的一种查尔酮，具有保护肝脏的作用。4′-Hydroxychalcone 能通过抑制蛋白酶体 (proteasome)，抑制TNFα 诱导的 NF-κB 活性。4′-Hydroxychalcone 能诱导大鼠离体肝线粒体囊泡快速释放钾，并引起其线粒体呼吸控制和氧化磷酸化衰退。

4

4′-Hydroxychalcone Chemical Structure

CAS No. : 2657-25-2

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10 mM * 1 mL in DMSO ￥660 In-stock
100 mg ￥600 In-stock
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生物活性

4′-Hydroxychalcone is a chalcone isolated from licorice root, with hepatoprotective activity. 4′-Hydroxychalcone inhibits TNFα-induced NF-κB activation via proteasome inhibition. 4′-Hydroxychalcone induces a rapid potassium release from mitochondrial vesicles and causes deterioration of respiratory control and oxidative phosphorylation of isolated rat liver mitochondria[1][2][3].

体外研究
(In Vitro)

4′-Hydroxychalcone (20-40 μM ; 2 hours) inhibits TNFα-induced (20 ng/mL; 6 hours) NF-kB pathway activation in a dose-dependent manner[3].
4′-Hydroxychalcone (0.1-25 μM ; 8 hours) inhibits proteasome activity in a dose-dependent manner but has no effect on IKK activity[3].
4′-Hydroxychalcone inhibits TNFα-dependent degradation of IkBα and subsequently prevents p50/p65 nuclear translocation leading to 4′-Hydroxychalcone-inhibited expression of NF-kB target genes[3].
4′-Hydroxychalcone affects cancer cell viability but has no significant effect on non-transformed cell viability[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[3]

Cell Line: K562 cells, Jurkat cells, U937 cells, PBMCs
Concentration: 5 μM, 10 μM, 20 μM, 24 μM, 28 μM, 32 μM, 40 μM, 60 μM
Incubation Time: 24 hours
Result: Affected cancer cell viability but has no significant effect on non-transformed cell viability.

Western Blot Analysis[3]

Cell Line: Jurkat cells
Concentration: 60 μM (followed by TNFα 20 ng/mL )
Incubation Time: 2 hours
Result: Inhibited TNFα -dependent degradation of IkBα and prevents p50/p65 nuclear translocation.

体内研究
(In Vivo)

4′-Hydroxychalcone has hepatoprotective activity against Acetaminophen induced hepatotoxicity in mice[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male albino mice(5-30 g)[2]
Dosage: 25 mg/kg, 50 mg/kg, 100 mg/kg
Administration: Oral administration, 12h intervals, 4 doses
Result: Significantly reduced the mortality rate induced by Acetaminophen (1 g/kg).

分子量

224.25

Formula

C15H12O2
CAS 号

2657-25-2
中文名称

4′-羟基查耳酮
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 : 250 mg/mL (1114.83 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.4593 mL 22.2965 mL 44.5931 mL
5 mM 0.8919 mL 4.4593 mL 8.9186 mL
10 mM 0.4459 mL 2.2297 mL 4.4593 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 (9.28 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (9.28 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 (9.28 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (9.28 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 (9.28 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (9.28 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 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Inoue B, et al. The effects of echinatin and its related compounds on the mitochondrial energy transfer reaction. J Toxicol Sci. 1982 Nov;7(4):245-54.

    [2]. Ali Reza, et al. Hepatoprotective activity of phloretin and hydroxychalcones against Acetaminophen Induced hepatotoxicity in mice. Iranian Journal of Pharmaceutical Sciences. 2011 Jan; 7(2).

    [3]. Orlikova B, et al. The aromatic ketone 4′-hydroxychalcone inhibits TNFα-induced NF-κB activation via proteasome inhibition. Biochem Pharmacol. 2011 Sep 15;82(6):620-31.

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