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Fenofibric acid [42017-89-0]

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Référence HY-B0760-500mg

Conditionnement : 500mg

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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.

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Fenofibric acid Chemical Structure

CAS No. : 42017-89-0

This product is a controlled substance and not for sale in your territory.

Based on 1 publication(s) in Google Scholar

Other Forms of Fenofibric acid:

Choline Fenofibrate In-stock
Fenofibric acid-d₆ Obtenir un devis
Fenofibric acid (Standard) Obtenir un devis

Voir tous les produits spécifiques à Isoform PPAR:

Voir toutes les isoformes

PPARα PPARβ/δ PPARγ PPAR PPARδ

Voir tous les produits spécifiques à Isoform COX:

Voir toutes les isoformes

COX COX-1 COX-2 COX-3

Description

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.

Essai clinique

Masse moléculaire

318.75

Formule

C₁₇H₁₅ClO₄

CAS No.

42017-89-0

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

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvant et solubilité

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
10 mM	0.3137 mL	1.5686 mL	3.1373 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.

Calculateur de molarité
Calculateur de dilution

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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)

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.

Pureté et documentation

Purity: 99.94%

Select Batch:

SDS (596 KB)

COA (245 KB) RP-HPLC (205 KB)

Instruction de manipulation (2659 KB)

Références

[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]

Test cellulaire ^[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 n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
Administration animale ^[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 n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
Références	[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

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

Fenofibric acid Related Classifications

Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease Immunology/Inflammation
PPAR COX

Fenofibric acid [42017-89-0]

Référence HY-B0760-500mg

Contactez votre distributeur local :

Marque : MedChemExpress

Contactez votre distributeur local :

Other Forms of Fenofibric acid:

Voir tous les produits spécifiques à Isoform PPAR:

Voir tous les produits spécifiques à Isoform COX:

Calculateur de molarité

Calculateur de dilution

Complete Stock Solution Preparation Table

Fenofibric acid Related Classifications

Keywords:

Vous serez peut-être également intéressé par les produits suivants :

Fenofibric acid [42017-89-0]

Référence HY-B0760-500mg

Contactez votre distributeur local :

Marque : MedChemExpress

Contactez votre distributeur local :

Other Forms of Fenofibric acid:

Voir tous les produits spécifiques à Isoform PPAR:

Voir tous les produits spécifiques à Isoform COX:

Fenofibric acid Related Antibodies

Calculateur de molarité

Calculateur de dilution

Complete Stock Solution Preparation Table

Fenofibric acid Related Classifications

Keywords:

Vous serez peut-être également intéressé par les produits suivants :