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.
For research use only. We do not sell to patients.
Nobiletin Chemical Structure
CAS No. : 478-01-3
This product is a controlled substance and not for sale in your territory.
Nobiletin (Nob; 100 mg/kg/day; s.c.; 10 weeks) markedly reduces D-gal (D-galactose)-induced increases in the ratio of p-FOXO 3a/FOXO and the expression of MAFbx and MuRF1 in mice.
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Description
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].
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Nobiletin Related Antibodies
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.
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].
MedChemExpress (MCE) 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.
Room temperature in continental US; may vary elsewhere.
Storage
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
1 year
-20°C
6 months
Solvent & Solubility
In Vitro:
DMSO : 50 mg/mL (124.26 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Preparing Stock Solutions
ConcentrationSolventMass
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
View the Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Protocol 1
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.21 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 2
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 3
Add each solvent one by one: 10% DMSO 90% Corn Oil
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (20.8 mg/mL) to 900 μLCorn oil, and mix evenly.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
[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.
[Content Brief]
[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.
[Content Brief]
[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.
[Content Brief]
[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.
[Content Brief]
[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.
Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Optional Solvent
ConcentrationSolventMass
1 mg
5 mg
10 mg
25 mg
DMSO
1 mM
2.4852 mL
12.4258 mL
24.8515 mL
62.1288 mL
5 mM
0.4970 mL
2.4852 mL
4.9703 mL
12.4258 mL
10 mM
0.2485 mL
1.2426 mL
2.4852 mL
6.2129 mL
15 mM
0.1657 mL
0.8284 mL
1.6568 mL
4.1419 mL
20 mM
0.1243 mL
0.6213 mL
1.2426 mL
3.1064 mL
25 mM
0.0994 mL
0.4970 mL
0.9941 mL
2.4852 mL
30 mM
0.0828 mL
0.4142 mL
0.8284 mL
2.0710 mL
40 mM
0.0621 mL
0.3106 mL
0.6213 mL
1.5532 mL
50 mM
0.0497 mL
0.2485 mL
0.4970 mL
1.2426 mL
60 mM
0.0414 mL
0.2071 mL
0.4142 mL
1.0355 mL
80 mM
0.0311 mL
0.1553 mL
0.3106 mL
0.7766 mL
100 mM
0.0249 mL
0.1243 mL
0.2485 mL
0.6213 mL
Nobiletin Related Classifications
Help & FAQs
Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.