Fenofibric acid
Based on 3 publication(s) in Google Scholar
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.
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- 純度: 99.94%
- CAS 番号: 42017-89-0
- 分子式: C17H15ClO4
- 分子量:318.76
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Fenofibric acid
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生物活性
製品説明
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PPARδ 1.06 μM (EC50) |
PPARγ 1.47 μM (EC50) |
PPARα 22.4 μM (EC50) |
COX-2 48 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BHK-21 | EC50 |
217 μM
Compound: Fenofibric acid
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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
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[PMID: 19349176] |
| CHO | EC50 |
12 μM
Compound: Fenofibric acid
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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
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[PMID: 21377875] |
| COS-1 | EC50 |
12 μM
Compound: Fenofibric acid
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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
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[PMID: 21130649] |
| CV-1 | EC50 |
18 μM
Compound: 2b
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Compound was tested for its agonist activity against murine Peroxisome proliferator activated receptor alpha-Gal4 chimeric receptor transfected CV-1 cells
Compound was tested for its agonist activity against murine Peroxisome proliferator activated receptor alpha-Gal4 chimeric receptor transfected CV-1 cells
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[PMID: 10508427] |
| CV-1 | EC50 |
250 μM
Compound: 2b
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Compound was tested for its agonist activity against murine Peroxisome proliferator activated receptor gamma-Gal4 chimeric receptor in transfected CV-1 cells
Compound was tested for its agonist activity against murine Peroxisome proliferator activated receptor gamma-Gal4 chimeric receptor in transfected CV-1 cells
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[PMID: 10508427] |
| CV-1 | EC50 |
30 μM
Compound: 2b
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Compound was tested for agonist activity on human Peroxisome proliferator activated receptor alpha-Gal4 chimeric receptor in transfected CV-1 cells
Compound was tested for agonist activity on human Peroxisome proliferator activated receptor alpha-Gal4 chimeric receptor in transfected CV-1 cells
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[PMID: 10508427] |
| CV-1 | EC50 |
300 μM
Compound: 2b
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Compound was tested for agonist activity on human Peroxisome proliferator activated receptor gamma-Gal4 chimeric receptor in transfected CV-1 cells
Compound was tested for agonist activity on human Peroxisome proliferator activated receptor gamma-Gal4 chimeric receptor in transfected CV-1 cells
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[PMID: 10508427] |
| CV-1 | EC50 |
2646 nM
Compound: 1b, Fenofibric acid
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Activity at human PPARalpha in CV1 cells
Activity at human PPARalpha in CV1 cells
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[PMID: 17005394] |
| CV-1 | EC50 |
>100 μM
Compound: fenofibric acid
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Agonist activity at human PPARalpha expressed in CV1 cells by transactivation assay
Agonist activity at human PPARalpha expressed in CV1 cells by transactivation assay
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[PMID: 17964792] |
| CV-1 | EC50 |
>100 μM
Compound: fenofibric acid
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Agonist activity at human PPARdelta expressed in CV1 cells by transactivation assay
Agonist activity at human PPARdelta expressed in CV1 cells by transactivation assay
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[PMID: 17964792] |
| CV-1 | EC50 |
100 μM
Compound: fenofibric acid
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Agonist activity at human PPARgamma expressed in CV1 cells by transactivation assay
Agonist activity at human PPARgamma expressed in CV1 cells by transactivation assay
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[PMID: 17964792] |
| CV-1 | EC50 |
>100 μM
Compound: 1b, fenofibric acid
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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
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[PMID: 18280733] |
| CV-1 | EC50 |
>100 μM
Compound: 1b, fenofibric acid
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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
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[PMID: 18280733] |
| CV-1 | EC50 |
30 μM
Compound: 1b, fenofibric acid
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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
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[PMID: 18280733] |
| HEK293 | EC50 |
9.2 μM
Compound: 13, FA
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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
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[PMID: 16617018] |
| HEK293 | EC50 |
>10 μM
Compound: fenofibricacid
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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
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[PMID: 17343371] |
| HEK293 | EC50 |
>10 μM
Compound: fenofibricacid
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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
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[PMID: 17343371] |
| HepG2 | EC50 |
30 μM
Compound: fenofibric acid
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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
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[PMID: 19775169] |
| HepG2 | EC50 |
300 μM
Compound: fenofibric acid
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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
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[PMID: 19775169] |
| L6 | EC50 |
3 μM
Compound: fenofibricacid
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Effect on fatty acid oxidation in rat L6 cells
Effect on fatty acid oxidation in rat L6 cells
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[PMID: 17343371] |
| Sf9 | IC50 |
950 μM
Compound: 20
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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
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[PMID: 27046190] |
体外実験
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.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 42017-89-0
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性状 Solid
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分子量 318.76
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分子式 C17H15ClO4
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Color White to off-white
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SMILES
CC(C)(OC1=CC=C(C(C2=CC=C(Cl)C=C2)=O)C=C1)C(O)=O
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別名
フェノフィブリン酸; FNF acid
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Cell Metab
The enedioic acid analog 326E alleviates metabolic dysfunction-associated steatohepatitis via dual targeting at ACLY and PPARα. [Abstract]2025 Oct 22:S1550-4131(25)00396-1. PMID: 41130202 -
Br J Pharmacol
Fenofibrate potentiates the therapeutic efficacy of EZH2 inhibitors on melanoma via TRIM21- and OTUD4-mediated EZH2 ubiquitination. [Abstract]2026 Jun;183(11):2675-2694. PMID: 41652905 -
Eur J Med Chem
Design, synthesis and anti-diabetic evaluation of novel PPAR agonists based on functional group-oriented strategy. [Abstract]2025 Oct 9:301:118226. PMID: 41075607
溶剤 & 溶解度
体外:
DMSO : ≥ 100 mg/mL (313.72 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.
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
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.
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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
プロトコル
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].
MedChemExpress (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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (278 KB)
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SDS (597 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Dietz M, et al. Comparative molecular profiling of the PPARα/γ activator aleglitazar: PPAR selectivity, activity and interaction with cofactors. ChemMedChem. 2012 Jun;7(6):1101-11. [Content Brief]
[2]. Prasad GS, et al. Anti-inflammatory activity of anti-hyperlipidemic drug, fenofibrate, and its phase-I metabolite fenofibric acid: in silico, in vitro, and in vivo studies. Inflammopharmacology. 2017 Dec 13. [Content Brief]
[3]. Neumeier M, et al. Aldehyde oxidase 1 is highly abundant in hepatic steatosis and is downregulated by adiponectin and fenofibric acid in hepatocytes in vitro. Biochem Biophys Res Commun. 2006 Nov 24;350(3):731-5. Epub 2006 Sep 27. [Content Brief]
[4]. Miranda S, et al. Beneficial effects of fenofibrate in retinal pigment epithelium by the modulation of stress and survival signaling under diabetic conditions. J Cell Physiol. 2012 Jun;227(6):2352-62. [Content Brief]
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 | 3.1372 mL | 15.6858 mL | 31.3716 mL | 78.4289 mL |
| 5 mM | 0.6274 mL | 3.1372 mL | 6.2743 mL | 15.6858 mL | |
| 10 mM | 0.3137 mL | 1.5686 mL | 3.1372 mL | 7.8429 mL | |
| 15 mM | 0.2091 mL | 1.0457 mL | 2.0914 mL | 5.2286 mL | |
| 20 mM | 0.1569 mL | 0.7843 mL | 1.5686 mL | 3.9214 mL | |
| 25 mM | 0.1255 mL | 0.6274 mL | 1.2549 mL | 3.1372 mL | |
| 30 mM | 0.1046 mL | 0.5229 mL | 1.0457 mL | 2.6143 mL | |
| 40 mM | 0.0784 mL | 0.3921 mL | 0.7843 mL | 1.9607 mL | |
| 50 mM | 0.0627 mL | 0.3137 mL | 0.6274 mL | 1.5686 mL | |
| 60 mM | 0.0523 mL | 0.2614 mL | 0.5229 mL | 1.3071 mL | |
| 80 mM | 0.0392 mL | 0.1961 mL | 0.3921 mL | 0.9804 mL | |
| 100 mM | 0.0314 mL | 0.1569 mL | 0.3137 mL | 0.7843 mL |
Fenofibric acid 関連分類
HY-B0760 関連分類
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