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Magnolol, a natural lignan isolated from the stem bark of Magnolia officinalis, is a dual agonist of both RXRα and PPARγ, with EC50 values of 10.4 µM and 17.7 µM, respectively.

For research use only. We do not sell to patients.

Magnolol Chemical Structure

Magnolol Chemical Structure

CAS No. : 528-43-8

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Customer Review

Based on 2 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

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Description

Magnolol, a natural lignan isolated from the stem bark of Magnolia officinalis, is a dual agonist of both RXRα and PPARγ, with EC50 values of 10.4 µM and 17.7 µM, respectively.

IC50 & Target[1]

PPARγ

17.7 μM (EC50)

In Vitro

Magnolol is a dual agonist of both RXRα and PPARγ, with EC50 values of 10.4 µM and 17.7 µM, respectively. Magnolol (26.2-80 µM) binds to RXRαLBD and PPARγLBD in a dose dependent manner, with Kd values of 45.7 µM and 1.67 µM, respectively. Magnolol (1-20 µM) induces the transcription of PPRE in a dose-dependent manner, but shows no activity on RXRE transcription[1]. Magnolol (1, 3, 10 µM) enhances adipocyte differentiation of both 3T3-L1 pre-adipocystes and C3H10T1/2 pluripotent stem cells in the presence of insulin. Magnolol (10 μM) upregulates mRNA expression of marker genes for adipocyte differentiation. Magnolol (1, 10 μM) shows an increase in basal and insulin-stimulated glucose uptake in differentiated 3T3-L1 adipocytes[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Magnolol (5-15 mg/kg, p.o.) significantly attenuates the phenotypic severity of dextran sulfate sodium (DSS)-induced colitis in mice. Magnolol (10, 15 mg/kg, p.o.) attenuates histopathological changes and myeloperoxidase activity in the colon of DSS-treated mice, decreases DSS-induced high levels of proinflammatory cytokines TNF-α, IL-1β and IL-6 in the colonic tissues. Magnolol (10 mg/kg, p.o.) also reverses abnormality of serum metabolome, and regulates tryptophan metabolic pathway in mice[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

266.33

Formula

C18H18O2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC1=CC=C(CC=C)C=C1C2=CC(CC=C)=CC=C2O

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (375.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.7547 mL 18.7737 mL 37.5474 mL
5 mM 0.7509 mL 3.7547 mL 7.5095 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (9.39 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 μL DMSO stock solution (25.0 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 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (9.39 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 μL DMSO 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.
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.
 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.
Purity & Documentation

Purity: 99.92%

References
Kinase Assay
[1]

Binding affinities of magnolol towards purified RXRαLBD and PPARγLBD are analyzed using Biacore 3000 instrument. Proteins are covalently immobilized to CM5 chip using a standard amine-coupling procedure in 10 mM sodium acetate buffer (pH 4.2). The chip is equilibrated with a continuous flow of running buffer (10 mM HEPES, pH 7.4, 150 mM NaCl, 3 mM EDTA, 0.005% (v/v) surfactant P20) for 2 hours. Subsequently, magnolol in a gradient of concentrations are injected into the channels at a flow rate of 20 µL/min for 60 seconds, followed by disassociation for 120 seconds. For the coactivator SRC1 recruitment assays, biotin-labelled SRC1 is immobilized to SA chip. Different concentrations of Magnolol are incubated with 5 µM RXRαLBD or PPARγLBD for 1 hour, and then injected to the channel at a flow rate of 20 µL/min for 60 s, followed by disassociation for 120 s[1].

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

Cell Assay
[2]

For differentiation of 3T3-L1 pre-adipocytes, at 2 days after confluence (defined as day 0), cells are incubated in differentiation medium containing 0.5 mM IBMX, 10 μg/mL insulin and 0.25 μM DEX in DMEM containing 10% fetal bovine serum (FBS). After 2 days, the cell culture medium is changed to DMEM containing 10 μg/mL insulin and 10% FBS. The medium is replaced again with fresh DMEM containing 10% FBS after 2 days. Adipocytes are used 6-8 days after the initiation of differentiation. In adipogenesis studies, 3T3-L1 pre-adipocytes and C3H10T1/2 pluripotent stem cells grown in DMEM supplemented with 10% bovine calf serum (day 0) are treated with insulin (1 μg/mL) with/without Magnolol in 10% FBS contained DMEM at the indicated concentration for 9 days. Fresh medium containing insulin (1 μg/mL) and 10% FBS with/without magnolol is replenished every 3 days[2].

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

Animal Administration
[3]

Experimental colitis mice model is induced by routine administration of dextran sulfate sodium (DSS) solution dissolved in drinking distilled water at a concentration of 2.0% (w/v) ad libitum for 5 consecutive days. Distilled water is given to mice in the normal group for the same period. The body weight of each mice is recorded daily in the morning (9:00 a.m.). On day 6, the mice with significant body weight loss, diarrhea, and gross bleeding are considered as experimental candidates of colitis. All the mice with comparable disease index are then randomly divided into 5 groups (n = 8/group): (1) DSS model group, intragastric administrated with saline; (2) positive control group, intraperitoneal injected with infliximab (5 mg/kg); (3) low dose treatment group, intragastric administrated with Magnolol (5 mg/kg); (4) medium dose treatment group, intragastric administrated with Magnolol (10 mg/kg); (5) high dose treatment group, intragastric administrated with Magnolol (15 mg/kg). The mice in control group receives drinking water without DSS throughout the entire experimental period and intragastric administrated with saline[3].

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

References

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.7547 mL 18.7737 mL 37.5474 mL 93.8685 mL
5 mM 0.7509 mL 3.7547 mL 7.5095 mL 18.7737 mL
10 mM 0.3755 mL 1.8774 mL 3.7547 mL 9.3869 mL
15 mM 0.2503 mL 1.2516 mL 2.5032 mL 6.2579 mL
20 mM 0.1877 mL 0.9387 mL 1.8774 mL 4.6934 mL
25 mM 0.1502 mL 0.7509 mL 1.5019 mL 3.7547 mL
30 mM 0.1252 mL 0.6258 mL 1.2516 mL 3.1290 mL
40 mM 0.0939 mL 0.4693 mL 0.9387 mL 2.3467 mL
50 mM 0.0751 mL 0.3755 mL 0.7509 mL 1.8774 mL
60 mM 0.0626 mL 0.3129 mL 0.6258 mL 1.5645 mL
80 mM 0.0469 mL 0.2347 mL 0.4693 mL 1.1734 mL
100 mM 0.0375 mL 0.1877 mL 0.3755 mL 0.9387 mL
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  • 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.

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