1. Metabolic Enzyme/Protease
    NF-κB
    Cell Cycle/DNA Damage
    Autophagy
  2. Cytochrome P450
    PPAR
    Autophagy

Fenofibrate 

Cat. No.: HY-17356 Purity: 99.92%
Data Sheet SDS Handling Instructions

Fenofibrate is a relatively potent inhibitor of CYP2C19 (IC50=0.2 μM) and CYP2B6 (IC50=0.7 μM). Fenofibrate is also a well-known PPARα agonist (EC50=30 μM).

For research use only. We do not sell to patients.
Fenofibrate Chemical Structure

Fenofibrate Chemical Structure

CAS No. : 49562-28-9

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $55 In-stock
5 g $50 In-stock
10 g $60 In-stock
50 g   Get quote  

* Please select Quantity before adding items.

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Fenofibrate is a relatively potent inhibitor of CYP2C19 (IC50=0.2 μM) and CYP2B6 (IC50=0.7 μM). Fenofibrate is also a well-known PPARα agonist (EC50=30 μM).

IC50 & Target

IC50: 0.2 μM (CYP2C19), 0.7 μM (CYP2B6)[1]
EC50: 2.39±0.4 μM (CYP2C), 30 μM (PPARα)[2]

In Vitro

Fenofibrate is a relatively potent inhibitor of CYP2B6 (IC50=0.7±0.2 μM) and CYP2C19 (IC50=0.2±0.1 μM). Fenofibrate is also a moderate inhibitor of CYP2C8 (IC50=4.8±1.7 μM) and CYP2C9 (IC50=9.7 μM)[1]. Fenofibrate binds to and inhibits cytochrome P450 epoxygenase (CYP)2C with higher affinity than to PPARα. Fenofibrate is a well-known PPARα agonist, but an in vitro assessment of 209 frequently prescribed drugs and related xenobiotics suggests that Fenofibrate is also a potent inhibitor of cytochrome P450 epoxygenase (CYP)2C. The affinity of Fenofibrate to CYP2C is >10 times higher (EC50=2.39±0.4 μM) than to PPARα (EC50=30 μM). Fenofibrate at a low dose inhibits CYP2C8 activity without PPARα activation[2].

In Vivo

Daily intake of Fenofibrate at this low dose (10 μg/g/day) inhibits retinal and choroidal neovascularization induced by CYP2C8 overexpression by 29% (P=0.021) and 36% (P=1.2×10−9) respectively[2].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT01965834 University of Miami Multiple Myeloma November 19, 2012 Phase 2
NCT02314533 Beijing Chao Yang Hospital Microalbuminuria December 2014 Phase 4
NCT00246636 GlaxoSmithKline Hypertriglyceridemia October 2005 Phase 4
NCT01023750 University of Alabama at Birmingham|Tufts University|University of Minnesota - Clinical and Translational Science Institute Hypertriglyceridemia|Insulin Resistance January 2010 Phase 4
NCT00961116 Mutual Pharmaceutical Company, Inc. Healthy October 2007 Phase 1
NCT00960687 Mutual Pharmaceutical Company, Inc. Healthy October 2007 Phase 1
NCT01462877 Abbott|Rundo International Pharmaceutical Research & Development Co.,Ltd. Dyslipidemias|Cardiovascular Diseases|Hypertriglyceridemia October 2011 Phase 4
NCT01878227 Zhejiang University Hyperlipoproteinemia July 2010 Phase 3
NCT00613613 University of Minnesota - Clinical and Translational Science Institute|Laval University Dyslipidemia January 2008 Phase 4
NCT00552747 National Heart Institute, Mexico Coronary Heart Disease|Hyperlipidemia October 2007 Phase 4
NCT00928694 Merck Sharp & Dohme Corp. Dyslipidemia February 2003 Phase 1
NCT01142323 University of Miami|University of Florida Primary Sclerosing Cholangitis October 2010 Phase 1|Phase 2
NCT01280604 Kaiser Permanente Hyperlipidemias October 2010
NCT00813527 Takeda Hyperlipidemias February 2006 Phase 2
NCT02232360 Gachon University Gil Medical Center|Daewoong Pharmaceutical Co. LTD. Coronary Artery Disease January 2014 Phase 3
NCT02886299 Cairo University Fenofibrate/Simvastatin Comparison October 2013 Phase 4
NCT02965911 Beijing 302 Hospital Primary Biliary Cirrhosis January 2016 Phase 1|Phase 2
NCT00872599 Vanderbilt University|National Institutes of Health (NIH) Hypertension September 2009 Phase 4
NCT00819910 Ahmad Slim|GlaxoSmithKline|Brooke Army Medical Center Hypertriglyceridemia in Type 4 Hyperlipidemia|Non Diabetic Subjects With Normoglycemia September 2008 Phase 4
NCT00816829 Solvay Pharmaceuticals Dyslipidemia|Sleep Apnea Syndrome|Overweight|Obesity September 2005 Phase 2
NCT00575042 University of Florida|The PBCers Organization|Shionogi Inc. Primary Biliary Cirrhosis August 2007 Phase 2
NCT00775359 Ranbaxy Laboratories Limited|Ranbaxy Inc. Healthy August 2002
NCT00775827 Ranbaxy Laboratories Limited|Ranbaxy Inc. Healthy November 2002
NCT01109758 Solvay Pharmaceuticals Healthy March 2008 Phase 1
NCT02823353 Xijing Hospital of Digestive Diseases Primary Biliary Cirrhosis January 2016 Phase 3
NCT01574131 The University of Texas Medical Branch, Galveston|Shriners Hospitals for Children Second or Third Degree Burns May 2012 Phase 4
NCT02455336 VA Office of Research and Development Spinal Cord Injury|Dyslipidemia May 18, 2015 Phase 2|Phase 3
NCT02153879 Institut Investigacio Sanitaria Pere Virgili|Spanish Biomedical Research Centre in Diabetes and Associated Metabolic Disorders Type 2 Diabetes Mellitus|Dyslipidemia February 2009 Phase 4
NCT00644592 University of Florida|American College of Clinical Pharmacy Healthy March 2008
NCT00459745 Shionogi Inc.|Integrium Combined Hyperlipidemia April 2007 Phase 3
NCT02262143 IlDong Pharmaceutical Co Ltd Mixed Dyslipidemias November 2014 Phase 3
NCT00891293 GlaxoSmithKline Hypertriglyceridemia March 2006 Phase 4
NCT00673881 Radiant Research Dyslipidemia March 2008 Phase 1|Phase 2
NCT01320345 University of Sydney|Abbott|University of Melbourne|St Vincent's Hospital Melbourne|Melbourne Health|Royal Prince Alfred Hospital, Sydney, Australia Type 1 Diabetes Mellitus|Retinopathy|Diabetic Nephropathy September 2011 Phase 3
NCT01048502 University of Pennsylvania|National Heart, Lung, and Blood Institute (NHLBI)|GlaxoSmithKline Cardiovascular Disease January 2010
NCT02015988 Koval' O., MD|Dnipropetrovsk State Medical Academy Acute Coronary Syndrome|Diabetes Mellitus, Type 2|Hypertriglyceridemia January 2014 Phase 4
NCT01141296 University of Miami|Mayo Clinic Primary Biliary Cirrhosis April 2011 Phase 2
NCT01956201 Chong Kun Dang Pharmaceutical Mixed Hyperlipidemia December 2013 Phase 3
NCT01927315 University of Padova|Azienda Ospedaliera di Padova Diabetes|Diabetic Retinopathy August 2013 Phase 4
NCT02306889 Ranbaxy Laboratories Limited|Ranbaxy Inc. Healthy January 2010
NCT00349284 Solvay Pharmaceuticals Hyperlipidemia Combined January 2005 Phase 3
NCT00732485 The University of Texas Medical Branch, Galveston|Shriners Hospitals for Children Burn August 2008 Phase 2|Phase 3
NCT00884819 Lawson Health Research Institute Polycystic Ovary Syndrome December 2008
NCT02452255 The University of Texas Medical Branch, Galveston|National Institute of General Medical Sciences (NIGMS)|Shriners Hospitals for Children Burn November 2015 Phase 2|Phase 3
NCT00349375 Solvay Pharmaceuticals Hyperlipidemia November 2005 Phase 3
NCT00352183 Solvay Pharmaceuticals Cardiovascular Diseases January 2006 Phase 3
NCT02306902 Ranbaxy Laboratories Limited|Ranbaxy Inc. Healthy October 2009
NCT00965315 National Taiwan University Hospital Diabetes|CVD
NCT00362934 Solvay Pharmaceuticals Hyperlipidemia October 2006 Phase 3
NCT00362206 Solvay Pharmaceuticals Hyperlipidemia September 2006 Phase 3
NCT00632840 The University of Western Australia|National Heart Foundation, Australia Obesity|Lipid Disorders|Hypertriglyceridemia|Cardiovascular Disease June 2001 Phase 4
NCT00491400 Boston University Diabetes Mellitus|Metabolic Syndrome September 2005
NCT00422396 University of Michigan|Abbott Hypertriglyceridemia With the Metabolic Syndrome January 2001
NCT00400231 University of Pennsylvania|Abbott Metabolic Syndrome x August 2005 Phase 2
NCT00139061 Pfizer Hyperlipidemia March 2005 Phase 3
NCT02166593 Yooyoung Pharmaceutical Co.,Ltd. Combined Dyslipidemia May 2014 Phase 3
NCT00843661 Ospedale di Circolo - Fondazione Macchi|Merck Sharp & Dohme Corp. HIV|Hyperlipidemia|HIV Infections March 2009 Phase 4
NCT02823366 Xijing Hospital of Digestive Diseases Primary Biliary Cirrhosis January 2016 Phase 3
NCT01767610 Hanlim Pharm. Co., Ltd. Healthy Male Volunteers January 2013 Phase 1
NCT01010516 University of Ioannina Dyslipidemia October 2009 Phase 4
NCT00490178 Solvay Pharmaceuticals Diabetes Mellitus, Type 2|Dyslipidemia March 2007 Phase 3
NCT00006412 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections|Lipodystrophy Phase 3
NCT00186537 Stanford University|Abbott Insulin Resistance|Hypertriglyceridemia September 2003
NCT00349128 Solvay Pharmaceuticals Dyslipidemia/Glucose Metabolism Disorder January 2004 Phase 2|Phase 3
NCT00543647 Solvay Pharmaceuticals Healthy Volunteers August 2002 Phase 1
NCT01003847 Gachon University Gil Medical Center Hypertriglyceridemia November 2009 Phase 4
NCT00348725 Solvay Pharmaceuticals Dyslipidemia/Glucose Metabolism Disorder April 2005 Phase 3
NCT00745407 Gachon University Gil Medical Center Hypertriglyceridemia January 2005 Phase 4
NCT00076518 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections|Hypertriglyceridemia Phase 2
NCT01426438 AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID) HIV-1 Infection November 2011 Phase 2
NCT00376285 Pfizer Obesity November 2006 Phase 1
NCT01594983 Novartis Pharmaceuticals|Novartis Non Familial Chylocmicronemia Syndrome (Non-FCS) June 2012 Phase 2
NCT02354976 AstraZeneca Non-alcoholic Fatty Liver Disease (NAFLD|Hypertriglyceridemia September 2015 Phase 2
NCT00470262 VA Office of Research and Development Metabolic Syndrome X|Prediabetic State January 2007
NCT01723735 Sanofi|Regeneron Pharmaceuticals Hypercholesterolemia November 2012 Phase 1
NCT00349635 Solvay Pharmaceuticals Obesity October 2004 Phase 2
NCT00683176 Abbott Products|Abbott Diabetic Macular Edema September 2008 Phase 2
NCT00362765 Solvay Pharmaceuticals Type 2 Diabetes|Dyslipidemia October 2006 Phase 2|Phase 3
NCT01674712 Abbott Dyslipidemia June 2012 Phase 3
NCT01666041 Gachon University Gil Medical Center Hypertriglyceridemia January 2012 Phase 4
NCT00362323 Solvay Pharmaceuticals Dyslipidemia/Glucose Metabolism Disorder October 2006 Phase 3
NCT00385658 Novartis Dyslipidemia August 2006 Phase 4
NCT00361868 Solvay Pharmaceuticals Dyslipidemia|Glucose Metabolism Disorder June 2006 Phase 3
NCT00923676 Second University of Naples Sexual Dysfunction|Hyperlipidemia April 2008 Phase 4
NCT00195793 Abbott Hyperlipidemia August 2004 Phase 3
NCT02066207 Chong Kun Dang Pharmaceutical Dyslipidemia (Fredrickson Type Ⅱa)|Dyslipidemia (Fredrickson Type Ⅱb) March 2014 Phase 1
NCT00754039 Daiichi Sankyo Inc. Hypercholesterolemia|Hyperlipidemia, Familial Combined February 2003 Phase 4
NCT00261352 AstraZeneca Type 2 Diabetes March 2005 Phase 3
NCT00504829 Veloxis Pharmaceuticals Dyslipidemia July 2007 Phase 2
NCT00357500 Dana-Farber Cancer Institute|National Cancer Institute (NCI)|Boston Children’s Hospital Central Nervous System Tumor, Pediatric|Leukemia|Lymphoma|Neuroblastoma|Sarcoma|Unspecified Childhood Solid Tumor, Protocol Specific January 2005 Phase 2
NCT02158273 The Scripps Research Institute|National Institute on Alcohol Abuse and Alcoholism (NIAAA) Alcoholism May 2014 Phase 2
NCT00246376 Baylor College of Medicine|National Heart, Lung, and Blood Institute (NHLBI)|Legacy Community Health Center Cardiovascular Diseases|Heart Diseases|HIV Infections|Hyperlipidemia|Hypertriglyceridemia|Insulin Resistance|Atherosclerosis January 2004
NCT01539616 Cadila Healthcare Limited Hypertriglyceridemia|Dyslipidemia November 2011 Phase 2
NCT00703755 Solvay Pharmaceuticals Patients With Metabolic Syndrome March 2003 Phase 2
NCT00092560 Merck Sharp & Dohme Corp. Hypercholesterolemia|Hypertriglyceridemia December 2002 Phase 3
NCT00703482 Solvay Pharmaceuticals Patients With Type 2 Diabetes May 2003 Phase 2
NCT01752842 Washington University School of Medicine|National Institutes of Health (NIH)|National Heart, Lung, and Blood Institute (NHLBI)|Leducq Foundation Type II Diabetes Mellitus|Diabetes Complications March 2013
NCT00169559 GlaxoSmithKline Dyslipidaemias November 2003 Phase 2
NCT00809068 Keogh Institute for Medical Research HDL Cholesterol August 2005 Phase 4
NCT00092573 Merck Sharp & Dohme Corp. Hypercholesterolemia|Hypertriglyceridemia April 2003 Phase 3
NCT00361751 National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|Shriners Hospitals for Children Burns|Insulin Resistance May 2003 Phase 2
NCT00627653 National Institute on Aging (NIA) Cardiovascular Diseases October 2005
NCT01289639 VA Office of Research and Development Fatty Liver October 2005
NCT01101204 Medical University of Silesia Diabetes|Dyslipidemia|Inflammation|Cytokines July 2012
NCT00309712 Intermountain Health Care, Inc.|Abbott|Merck Sharp & Dohme Corp. Type II Diabetes Mellitus|Mixed Dyslipidemia August 2002
NCT00458055 McGill University Health Center Coronary Arteriosclerosis|Hypoalphalipoproteinemias|Genetic Diseases, Inborn November 2006
NCT00262964 Washington University School of Medicine|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) Non-Alcoholic Fatty Liver Disease October 2004
NCT00934258 National Taiwan University Hospital Hyperlipidemia
NCT00483210 University of Arkansas|National Institutes of Health (NIH) Tissue Lipid Metabolism
NCT00252499 VA Office of Research and Development Fatty Liver|Insulin Resistance October 2005
NCT00726856 Merck Sharp & Dohme Corp. Dyslipidemia May 2007
NCT00145431 Pfizer Hyperlipoproteinemia Type III March 2005 Phase 3
NCT01148004 National Institutes of Health Clinical Center (CC) HIV|Fenofibrate|Protease Inhibitors|Hypertriglyceridemia|Glucuronosyltransferase May 13, 2010 Phase 1
NCT00000620 National Heart, Lung, and Blood Institute (NHLBI)|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|National Institute on Aging (NIA)|National Eye Institute (NEI)|Centers for Disease Control and Prevention Atherosclerosis|Cardiovascular Diseases|Hypercholesterolemia|Hypertension|Diabetes Mellitus, Type 2|Diabetes Mellitus|Coronary Disease September 1999 Phase 3
NCT00304993 Foundation Research, Florida|GlaxoSmithKline|Kos Pharmaceuticals|Abbott Metabolic Syndrome X|Insulin Resistance January 2001 Phase 4
NCT00703690 Merck Sharp & Dohme Corp. Metabolic X Syndrome Dyslipidemia January 2002 Phase 2
NCT03011450 Kowa Research Institute, Inc. Severe Hypertriglyceridemia November 2016 Phase 3
NCT03001817 Kowa Research Institute, Inc. Severe Hypertriglyceridemia November 2016 Phase 3
NCT00559962 Aegerion Pharmaceuticals, Inc. Hyperlipidemia October 2007 Phase 2
NCT02642159 Sanofi|Regeneron Pharmaceuticals Dyslipidemia March 15, 2016 Phase 4
NCT00794963 Northwell Health Metabolic Syndrome November 2008
NCT02584504 Sanofi|Regeneron Pharmaceuticals Hypercholesterolaemia November 30, 2015 Phase 3
NCT00542178 National Heart, Lung, and Blood Institute (NHLBI)|National Eye Institute (NEI) Diabetic Retinopathy October 2003 Phase 3
NCT00673309 The University of Texas Medical Branch, Galveston|National Institutes of Health (NIH) Burns July 2002 Phase 2|Phase 3
NCT00359281 Aegerion Pharmaceuticals, Inc. Healthy March 2006 Phase 2
NCT02984982 Sanofi|Regeneron Pharmaceuticals Hypercholesterolemia|Acute Coronary Syndrome November 2016 Phase 4
NCT02890992 Sanofi|Regeneron Pharmaceuticals Hypercholesterolaemia September 2016 Phase 2
View MoreCollapse
References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 2.7714 mL 13.8569 mL 27.7139 mL
5 mM 0.5543 mL 2.7714 mL 5.5428 mL
10 mM 0.2771 mL 1.3857 mL 2.7714 mL
Kinase Assay
[1]

The half-maximal inhibitory concentrations (IC50s) of Fenofibrate, statins (atorvastatin, lovastatin, pravastatin, simvastatin and simvastatin acid, the active form of simvastatin) and glipizide for recombinant human CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and CYP3A4 are determined using fluorometric CYP450 inhibition assays. Briefly, the drugs are dissolved in methanol or acetonitrile. In 96 well assay plates, the drugs are diluted to a series of concentrations in a solution containing cofactors including NADP+ (final concentration 1.3 mM), MgCl2 (final concentration 3.3 m M), glucose-6-phosphate (G6P, final concentration 3.3 mM) and glucose 6-phosphate dehydrogenase (final concentration 0.4 U/mL). The mixture is pre-incubated at 37°C for 10 min. The enzymes and fluorogenic substrates are diluted to desired concentrations in sodium phosphate reaction buffer (pH 7.4, final concentration 200 mM) and mixed. Reactions are initiated with addition of the enzyme and substrate mixture to the cofactor and drug mixture. The final reaction volume of all assays is 200 μL. After incubating at 37°C for a pre-specified period of time (15 to 45 min), the reactions are stopped with addition of 75 μL quenching solution (0.5 M Tris base or 2N NaOH). Fluorescence is determined using a BioTek Synergy 2 fluorescence reader. Each of the drugs is tested at eight concentrations in duplicate. To estimate IC50s, percent of inhibition is calculated using net fluorescence that is corrected for the background. The values of percent of inhibition are then fitted to a three or four parameter log-logistic model[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

For the higher dose(100 mg/kg/day), Fenofibrate is dissolved in corn oil (Mice)[2].
For the lower dose treatment (10 mg/kg/day), Fenofibrate is dissolved in 10% DMSO to make a 10 mg/mL solution (Mice)[2].

Mice[2]
The mouse oxygen-induced retinopathy (OIR) model is used. Briefly to induce retinal neovascularization, mouse pups and their nursing mother are exposed to 75±3% oxygen from P7 to P12. For the higher dose Fenofibrate (F6020) treatment (100 mg/kg/day). Fenofibrate is dissolved in corn oil to make 100mg/mL solution and pure corn oil is used as vehicle control. For the lower dose treatment (10 mg/kg/day), Fenofibrate is dissolved in 10% DMSO, D2650 to make a 10 mg/mL solution and 10% DMSO is used as vehicle control. After return to room air, mice are orally gavaged with Fenofibrate (100 or 10 mg/kg) or vehicle control daily from P12 to P16. At P17, eyes are enucleated immediately after euthanasia and fixed in 4% paraformaldehyde in PBS for 1 h at room temperature. Retinas are then dissected and stained overnight with Alexa Fluor 594 conjugated isolectin GS-IB4 (10 μg/mL) at room temperature. After washing with PBS, retinas are mounted onto microscope slides with photoreceptor side down and embedded in SlowFade antifade mounting medium. Retinal images are taken using a fluorescence microscope with image software. Retinal neovascularization is analyzed. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

360.83

Formula

C₂₀H₂₁ClO₄

CAS No.

49562-28-9

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 47 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number

 

Organization name *

Country *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Fenofibrate
Cat. No.:
HY-17356
Quantity: