Nobiletin(Synonyms: 川陈皮素)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Nobiletin (Synonyms: 川陈皮素) 纯度: 99.52%

Nobiletin 是一种来自柑橘皮的聚甲氧基黄酮,可改善记忆力丧失,是一种 RORs 激动剂。Nobiletin 可以降低分化的 C2C12 肌管中的 ROS 的水平,并具有抗炎和抗癌特性,包括抗血管生成,抗增殖,抗转移和诱导细胞凋亡。

Nobiletin(Synonyms: 川陈皮素)

Nobiletin Chemical Structure

CAS No. : 478-01-3

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生物活性

Nobiletin is a poly-methoxylated flavone from the citrus peel that improves memory loss. Nobiletin is a retinoid acid receptor-related orphan receptors (RORs) agonist. Nobiletin can reduce reactive oxygen species (ROS) levels in differentiated C2C12 myotubes and has anti-inflammation and anti-cancer properties, including anti-angiogenesis, anti-proliferation, anti-metastasis and induced apoptosis[1][2][3][4].

IC50 & Target

Retinoid acid receptor-related orphan receptors (RORs)[1]; reactive oxygen species (ROS)[1]; apoptosis[2]

体外研究
(In Vitro)

Nobiletin (0-100 μM; 24 hours; U2OS and HOS cells) treatment progressively reduces protein expressions of MMP-2 and MMP-9. In U2OS and HOS cells, Nobiletin considerably reduces the phosphorylation of p-IKKα/β and p-IκBα, and protein expression of NF-κB in the cell nuclear fraction with the concomitant increase of the NF-κB expression in the cytosolic fraction. Nobiletin down-regulates the p-CREB and the SP-1 expressions in the nuclear fraction, whereas Nobiletin does not affect c-Jun and c-Fos expressions[1].
Nobiletin (0-100 μM; 24 hours; U2OS and HOS cells) treatment significantly reduces mRNA expressions of MMP-2 and MMP-9 dose-dependently in U2OS and HOS cells[1].

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.

Western Blot Analysis[1]

Cell Line: U2OS and HOS cells
Concentration: 0 μM, 25 μM, 50 μM, 75 μM, 100 μM
Incubation Time: 24 hours
Result: Progressively reduced protein expressions of MMP-2 and MMP-9. Considerably reduced the phosphorylation of p-IKKα/β and p-IκBα, and protein expression of NF-κB in the cell nuclear fraction with the concomitant increase of the NF-κB expression in the cytosolic fraction. Down-regulated the p-CREB and the SP-1 expressions in the nuclear fraction in U2OS and HOS cells.

RT-PCR[1]

Cell Line: U2OS and HOS cells
Concentration: 0 μM, 25 μM, 50 μM, 75 μM, 100 μM
Incubation Time: 24 hours
Result: Significantly reduced mRNA expressions of MMP-2 and MMP-9 dose-dependently in U2OS and HOS cells.

体内研究
(In Vivo)

Nobiletin (0.1% of regular diet; oral administration; daily; for 20 weeks; male C57BL/6 mice) treatment restores glucose homeostasis and promots energy expenditure and circadian activity in aged 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: 20- to 22-month-old male C57BL/6 mice[2]
Dosage: 0.1% of regular diet
Administration: Oral administration; daily; for 20 weeks
Result: Fully restored glucose tolerance in aged mice, and increased basal body temperature and cold tolerance in aged mice. Led to a twofold increase in distance run/day on voluntary wheels compared with aged regular diet-fed mice during the active phase.

分子量

402.39

Formula

C21H22O8

CAS 号

478-01-3

中文名称

蜜橘黄素;川皮亭;川皮苷;川陈皮素

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 : 50 mg/mL (124.26 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4852 mL 12.4258 mL 24.8515 mL
5 mM 0.4970 mL 2.4852 mL 4.9703 mL
10 mM 0.2485 mL 1.2426 mL 2.4852 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    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.21 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.21 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 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
  • 2.

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

    Solubility: ≥ 2.08 mg/mL (5.17 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.17 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

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (5.17 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.17 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]. Cheng HL, et al. Nobiletin inhibits human osteosarcoma cells metastasis by blocking ERK and JNK-mediated MMPs expression. Oncotarget. 2016 Jun 7;7(23):35208-23.

    [2]. Nohara K, et al. Nobiletin fortifies mitochondrial respiration in skeletal muscle to promote healthy aging against metabolic challenge. Nat Commun. 2019 Aug 28;10(1):3923.

    [3]. Takito J, et al. Nerve growth factor enhances the CRE-dependent transcriptional activity activated by nobiletin in PC12 cells. Can J Physiol Pharmacol. 2016 Jul;94(7):728-33.

    [4]. He B, et al. The Small Molecule Nobiletin Targets the Molecular Oscillator to Enhance Circadian Rhythms and Protect against Metabolic Syndrome. Cell Metab. 2016 Apr 12;23(4):610-21.

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