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  3. Eupatilin

Eupatilin, a lipophilic flavonoid isolated from Artemisia argyi, is a PPARα agonist, and possesses anti-apoptotic, anti-oxidative and anti-inflammatory activities.

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

Eupatilin Chemical Structure

Eupatilin Chemical Structure

CAS No. : 22368-21-4

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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Eupatilin:

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Eupatilin, a lipophilic flavonoid isolated from Artemisia argyi, is a PPARα agonist, and possesses anti-apoptotic, anti-oxidative and anti-inflammatory activities.

IC50 & Target[1]

PPARα

 

Cellular Effect
Cell Line Type Value Description References
A549 IC50
> 100 μM
Compound: 6
Cytotoxicity against human A549 cells assessed as reduction in cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as reduction in cell growth incubated for 48 hrs by MTT assay
[PMID: 27400887]
AGS IC50
0.5 x 10-4 M
Compound: Eupatilin
Antiproliferative activity against human AGS cells assessed as reduction in cell viability after 24 hrs by CCK8 assay
Antiproliferative activity against human AGS cells assessed as reduction in cell viability after 24 hrs by CCK8 assay
[PMID: 31784199]
Bcap37 IC50
> 100 μM
Compound: 6
Cytotoxicity against human Bcap37 cells assessed as reduction in cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against human Bcap37 cells assessed as reduction in cell growth incubated for 48 hrs by MTT assay
[PMID: 27400887]
HepG2 IC50
52.65 μM
Compound: 6
Cytotoxicity against human HepG2 cells assessed as reduction in cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell growth incubated for 48 hrs by MTT assay
[PMID: 27400887]
MCF7 IC50
90.07 μM
Compound: 6
Cytotoxicity against human MCF7 cells assessed as reduction in cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell growth incubated for 48 hrs by MTT assay
[PMID: 27400887]
MKN-1 IC50
0.5 x 10-4 M
Compound: Eupatilin
Antiproliferative activity against human MKN1 cells assessed as reduction in cell viability after 24 hrs by CCK8 assay
Antiproliferative activity against human MKN1 cells assessed as reduction in cell viability after 24 hrs by CCK8 assay
[PMID: 31784199]
SNU-638 IC50
0.5 x 10-4 M
Compound: Eupatilin
Antiproliferative activity against human SNU638 cells assessed as reduction in cell viability after 24 hrs by CCK8 assay
Antiproliferative activity against human SNU638 cells assessed as reduction in cell viability after 24 hrs by CCK8 assay
[PMID: 31784199]
T-cell IC50
11.7 μM
Compound: 16
Immunosuppressant activity in human T lymphocytes assessed as inhibition of anti-human CD3 and anti-human CD28 monoclonal antibody-induced T lymphocyte proliferation incubated for 72 hrs by FACS analysis
Immunosuppressant activity in human T lymphocytes assessed as inhibition of anti-human CD3 and anti-human CD28 monoclonal antibody-induced T lymphocyte proliferation incubated for 72 hrs by FACS analysis
[PMID: 31181920]
U-251 IC50
> 100 μM
Compound: 6
Cytotoxicity against human U251 cells assessed as reduction in cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against human U251 cells assessed as reduction in cell growth incubated for 48 hrs by MTT assay
[PMID: 27400887]
In Vitro

Eupatilin is a PPARα agonist. Eupatilin (10, 30, 100 μM) suppresses IL-4 expression and degranulation in RBL-2H3 cells[1]. Eupatilin (50-100 μM) slightly reduces cell viability of HaCaT cells. Eupatilin (10, 30, 50, 100 μM) increases PPARα transactivation and expression in HaCaT cells. Eupatilin (10, 30, 50 μM) also suppresses TNFα-induced MMP-2/-9 expression in HaCaT cells. Furthermore, Eupatilin inhibits TNFα-induced p65 translocation, IκBα Phosphorylation, AP-1 and MAPK signaling via PPARα[2]. Eupatilin (10-50 μM) shows no cytotoxic effects on ARPE19 cells. Eupatilin (10, 25, 50 μM) elevates cell viability from oxidative stress, and inhibits H2O2-induced ROS production in ARPE19 cells. Moreover, Eupatilin (50 μM) inbibits H2O2-induced cells apoptosis and promotes the activation of PI3K/Akt pathway in RPE cells[3].

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

In Vivo

Eupatilin (1.5% or 3.0%) restores PPARα mRNA expression, and improves atopic dermatitis (AD)-like symptoms in oxazolone-induced Balb/c mice. Eupatilin causes significant decrease in serum IgE, IL-4 levels, oxazolone-induced TNFα, IFNγ, IL-1β, TSLP, IL-33 and IL-25 mRNA expression in oxazolone-induced mice. Eupatilin also increases filaggrin and loricrin mRNA expression in oxazolone-induced mice[1].

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

Clinical Trial
Molecular Weight

344.32

Formula

C18H16O7

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C=C(C2=CC=C(OC)C(OC)=C2)OC3=CC(O)=C(OC)C(O)=C13

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (96.80 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 2.9043 mL 14.5214 mL 29.0428 mL
5 mM 0.5809 mL 2.9043 mL 5.8085 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 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

×
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 (7.26 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 (7.26 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: 98.90%

References
Cell Assay
[3]

Cell viability is detected using a MTT assay. In brief, after treatment, the medium is replaced with fresh medium containing 0.5 mg/mL MTT for 4 h at 37°C. Then, the medium is gently aspirated and 150 μL of DMSO is added to each well to solubilize the formazan crystals. The absorbance is measured at 450 nm by a microplate reader. The relative cell viability is defined as the absorbance of treated wells divided by that of the control[3].

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

Animal Administration
[1]

Six-week-old female Balb/c mice are housed under conditions of controlled temperature (23  ±  2 °C), humidity (55  ±  5%), and 12 h light/dark cycles (06:00-18:00 h light, 18:00-06:00 dark). Briefly, Balb/c mice are sensitized on day −7 by a single application of 20 μL of 1.0% oxazolone in a mixture of acetone and olive oil (4:1) to the inner and outer surface of both ears. On day 0, the mouse ears are challenged with 20 μL of 0.1% oxazolone at 2-day intervals for 4 weeks post-sensitization. The mice are treated with the indicated concentrations of Eupatilin (1.5% or 3.0%) twice a day for 4 weeks. The control group is treated with vehicle alone (acetone and olive oil [4:1]). After 3 weeks, the mice are sacrificed and samples are collected. Ears are stored at −80 °C for RNA isolation and analysis or immediately fixed in 4% formalin for histological analysis[1].

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9043 mL 14.5214 mL 29.0428 mL 72.6069 mL
5 mM 0.5809 mL 2.9043 mL 5.8086 mL 14.5214 mL
10 mM 0.2904 mL 1.4521 mL 2.9043 mL 7.2607 mL
15 mM 0.1936 mL 0.9681 mL 1.9362 mL 4.8405 mL
20 mM 0.1452 mL 0.7261 mL 1.4521 mL 3.6303 mL
25 mM 0.1162 mL 0.5809 mL 1.1617 mL 2.9043 mL
30 mM 0.0968 mL 0.4840 mL 0.9681 mL 2.4202 mL
40 mM 0.0726 mL 0.3630 mL 0.7261 mL 1.8152 mL
50 mM 0.0581 mL 0.2904 mL 0.5809 mL 1.4521 mL
60 mM 0.0484 mL 0.2420 mL 0.4840 mL 1.2101 mL
80 mM 0.0363 mL 0.1815 mL 0.3630 mL 0.9076 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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