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  3. Fenofibric acid

Fenofibric acid  (Synonyms: FNF acid)

Cat. No.: HY-B0760 Purity: 99.94%
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Fenofibric acid, an active metabolite of fenofibrate, is a PPAR activitor, with EC50s of 22.4 μM, 1.47 μM, and 1.06 μM for PPARα, PPARγ and PPARδ, respectively; Fenofibric acid also inhibits COX-2 enzyme activity, with an IC50 of 48 nM.

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

Fenofibric acid Chemical Structure

Fenofibric acid Chemical Structure

CAS No. : 42017-89-0

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Fenofibric acid:

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Fenofibric acid, an active metabolite of fenofibrate, is a PPAR activitor, with EC50s of 22.4 μM, 1.47 μM, and 1.06 μM for PPARα, PPARγ and PPARδ, respectively; Fenofibric acid also inhibits COX-2 enzyme activity, with an IC50 of 48 nM.

IC50 & Target[1][2]

PPARδ

1.06 μM (EC50)

PPARγ

1.47 μM (EC50)

PPARα

22.4 μM (EC50)

COX-2

48 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
BHK-21 EC50
217 μM
Compound: Fenofibric acid
Agonist activity at human PPARgamma expressed in BHK21 cells assessed as SEAP activity by luciferase reporter transactivation assay
Agonist activity at human PPARgamma expressed in BHK21 cells assessed as SEAP activity by luciferase reporter transactivation assay
[PMID: 19349176]
CHO EC50
12 μM
Compound: Fenofibric acid
Partial agonist activity at human PPARalpha expressed in CHO cells co-transfected with Gal4-responsive luciferase reporter plasmid after 24 hrs by transactivation assay
Partial agonist activity at human PPARalpha expressed in CHO cells co-transfected with Gal4-responsive luciferase reporter plasmid after 24 hrs by transactivation assay
[PMID: 21377875]
COS-1 EC50
12 μM
Compound: Fenofibric acid
Agonist activity at human PPARalpha ligand binding domain expressed in COS-1 cells co-transfected with Gal4 by luciferase reporter gene assay
Agonist activity at human PPARalpha ligand binding domain expressed in COS-1 cells co-transfected with Gal4 by luciferase reporter gene assay
[PMID: 21130649]
CV-1 EC50
> 100 μM
Compound: 1b, fenofibric acid
Agonist activity at human PPARgamma expressed in monkey CV1 cells by transactivation assay
Agonist activity at human PPARgamma expressed in monkey CV1 cells by transactivation assay
[PMID: 18280733]
CV-1 EC50
> 100 μM
Compound: 1b, fenofibric acid
Agonist activity at human PPARdelta expressed in monkey CV1 cells by transactivation assay
Agonist activity at human PPARdelta expressed in monkey CV1 cells by transactivation assay
[PMID: 18280733]
CV-1 EC50
> 100 μM
Compound: fenofibric acid
Agonist activity at human PPARalpha expressed in CV1 cells by transactivation assay
Agonist activity at human PPARalpha expressed in CV1 cells by transactivation assay
[PMID: 17964792]
CV-1 EC50
> 100 μM
Compound: fenofibric acid
Agonist activity at human PPARdelta expressed in CV1 cells by transactivation assay
Agonist activity at human PPARdelta expressed in CV1 cells by transactivation assay
[PMID: 17964792]
CV-1 EC50
100 μM
Compound: fenofibric acid
Agonist activity at human PPARgamma expressed in CV1 cells by transactivation assay
Agonist activity at human PPARgamma expressed in CV1 cells by transactivation assay
[PMID: 17964792]
CV-1 EC50
30 μM
Compound: 1b, fenofibric acid
Agonist activity at human PPARalpha expressed in monkey CV1 cells by transactivation assay
Agonist activity at human PPARalpha expressed in monkey CV1 cells by transactivation assay
[PMID: 18280733]
HEK293 EC50
> 10 μM
Compound: fenofibricacid
Activity at human liver PPAR alpha expressed in HEK293 cells by PPAR-GAL4 transactivation assay
Activity at human liver PPAR alpha expressed in HEK293 cells by PPAR-GAL4 transactivation assay
[PMID: 17343371]
HEK293 EC50
> 10 μM
Compound: fenofibricacid
Activity at human placenta PPAR delta expressed in HEK293 cells by PPAR-GAL4 transactivation assay
Activity at human placenta PPAR delta expressed in HEK293 cells by PPAR-GAL4 transactivation assay
[PMID: 17343371]
HEK293 EC50
9.2 μM
Compound: 13, FA
Agonist activity at human recombinant PPARalpha by transactivation of TK-MH100x4-LUC reporter gene in HEK293 cells
Agonist activity at human recombinant PPARalpha by transactivation of TK-MH100x4-LUC reporter gene in HEK293 cells
[PMID: 16617018]
HepG2 EC50
30 μM
Compound: fenofibric acid
Agonist activity at GAL4-tagged human PPARalpha ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation by luciferase reporter gene assay
Agonist activity at GAL4-tagged human PPARalpha ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation by luciferase reporter gene assay
[PMID: 19775169]
HepG2 EC50
300 μM
Compound: fenofibric acid
Agonist activity at GAL4-tagged human PPARgamma ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation by luciferase reporter gene assay
Agonist activity at GAL4-tagged human PPARgamma ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation by luciferase reporter gene assay
[PMID: 19775169]
Sf9 IC50
950 μM
Compound: 20
Inhibition of human recombinant COX1 expressed in Sf9 cell microsomes assessed as reduction in conversion of arachidonic acid to PGE2 incubated for 5 mins by HTRF assay
Inhibition of human recombinant COX1 expressed in Sf9 cell microsomes assessed as reduction in conversion of arachidonic acid to PGE2 incubated for 5 mins by HTRF assay
[PMID: 27046190]
In Vitro

Fenofibric acid is a PPAR activitor, with EC50s of 22.4 μM, 1.47 μM, and 1.06 μM for PPARα, PPARγ and PPARδ, respectively[1]. Fenofibric acid (10, 25, 50, 75, and 100 nM) dose-dependently inhibits COX-2 enzyme, with IC50 of 48 nM[2]. Fenofibric acid (500 nM) reduces abundance of AOX1 protein in HepG2 cells[3]. Fenofibric acid (100?μM) decreases JNK1/2, c-Jun, and p38 MAPK phosphorylation, and prevents the accumulation of reactive oxygen species, endoplasmic reticulum (ER) stress and disruption of blood retinal barrier (BRB) in response to the combination of high-glucose (HG) and hypoxia in ARPE-19 cells. Fenofibric acid (100?μM) activates IGF-IR/Akt/ERK1/2-mediated survival signaling pathways in ARPE-19 cells under HG conditions and hypoxia[4].

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

In Vivo

Fenofibric acid (1, 5, 10 mg/kg, p.o.) shows anti-inflammatory activity in Wistar rats with acute inflammation induced by carrageenan[2].

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

Clinical Trial
Molecular Weight

318.75

Formula

C17H15ClO4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(C)(OC1=CC=C(C(C2=CC=C(Cl)C=C2)=O)C=C1)C(O)=O

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 : ≥ 100 mg/mL (313.73 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1373 mL 15.6863 mL 31.3725 mL
5 mM 0.6275 mL 3.1373 mL 6.2745 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
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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 (7.84 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.84 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn 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 +
+
%
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%
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: 99.94%

References
Cell Assay
[4]

ARPE-19 cells are cultured under normoglycemic (5.5 mM D-glucose) or hyperglycemic (25 mM D-glucose) conditions for 18 days at 37°C under 5% (v/v) CO2 in medium DMEM/F12 supplemented with 10% (v/v) fetal serum (FS) and penicillin/streptomycin. ARPE-19 cells are used and the media is changed every 3-4 days. The conditions tested are: (1) Control cells which are maintained in 5.5 mM D-glucose (normal glucose) for 18 days. (2) Cells cultured in 5.5 mM D-glucose treated with 100 µM Fenofibric acid for 72 h (days 16, 17, and 18; 1 application/day). (3) Cells cultured as in (1) or (2) and submitted to hypoxia (1% oxygen) for the last 6 or 24 h. (4) Cells maintained in 25 mM D-glucose (HG) for 18 days. (5) Cells cultured in 25 mM D-glucose treated with 100 µM Fenofibric acid for 72 h (days 16, 17, and 18; 1 application/day). (6)Cells cultured as in (4) or (5) and submitted to hypoxia (1% oxygen) for the last 6 or 24 h[4].

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

Animal Administration
[2]

The anti-inflammatory activity of fenofibrate and its active metabolite fenofibric acid is assessed by injecting 0.1 mL of 1% carrageenan solution prepared in saline (sub-plantar) to the right hind paw of the rats. Rats are divided into 6 groups of six animals each. The first group serves as negative control and receives 1% tween-80 in distilled water, 10 mL/kg body mass. Group 2 and 3 receive a single dose of fenofibrate and standard drug diclofenac at 10 mg/kg body mass, whereas groups 4, 5, and 6 receive 3 doses of Fenofibric acid at 1, 5, and 10 mg/kg body mass, respectively. All the drugs are given orally using gavages 60 min before the injection of 0.1 mL of 1% carrageenan through sub-plantar route. The volume of oedema of test and control groups is measured using plethysmometer at 0, 1, 2, and 3 h after induction of inflammation[2].

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 3.1373 mL 15.6863 mL 31.3725 mL 78.4314 mL
5 mM 0.6275 mL 3.1373 mL 6.2745 mL 15.6863 mL
10 mM 0.3137 mL 1.5686 mL 3.1373 mL 7.8431 mL
15 mM 0.2092 mL 1.0458 mL 2.0915 mL 5.2288 mL
20 mM 0.1569 mL 0.7843 mL 1.5686 mL 3.9216 mL
25 mM 0.1255 mL 0.6275 mL 1.2549 mL 3.1373 mL
30 mM 0.1046 mL 0.5229 mL 1.0458 mL 2.6144 mL
40 mM 0.0784 mL 0.3922 mL 0.7843 mL 1.9608 mL
50 mM 0.0627 mL 0.3137 mL 0.6275 mL 1.5686 mL
60 mM 0.0523 mL 0.2614 mL 0.5229 mL 1.3072 mL
80 mM 0.0392 mL 0.1961 mL 0.3922 mL 0.9804 mL
100 mM 0.0314 mL 0.1569 mL 0.3137 mL 0.7843 mL
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Fenofibric acid
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