Synonym
Fenofibric Acid; Procetofenic acid; FNF Acid; NSC 281318; NSC281318; NSC-281318;
IUPAC/Chemical Name
2-[4-(4-chlorobenzoyl)phenoxy]-2-methylpropanoic acid
InChi Key
MQOBSOSZFYZQOK-UHFFFAOYSA-N
InChi Code
InChI=1S/C17H15ClO4/c1-17(2,16(20)21)22-14-9-5-12(6-10-14)15(19)11-3-7-13(18)8-4-11/h3-10H,1-2H3,(H,20,21)
SMILES Code
CC(C)(OC1=CC=C(C(C2=CC=C(Cl)C=C2)=O)C=C1)C(O)=O
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
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.
In vitro activity:
This finding showed that FF (fenofibrate) inhibits myofibroblast differentiation induced by TGF‐β. Moreover, treatment of IMR‐90 cells with TGF‐β increased the expression of CTGF (Fig. 1C), an important mediator of myofibroblast activation and extracellular matrix synthesis, and the production of collagen (Fig. 1D).
Reference: FEBS Open Bio. 2021 Aug; 11(8): 2340–2349. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8329776/
In vivo activity:
This finding showed that FF (fenofibrate) inhibits myofibroblast differentiation induced by TGF‐β. Moreover, treatment of IMR‐90 cells with TGF‐β increased the expression of CTGF (Fig. 1C), an important mediator of myofibroblast activation and extracellular matrix synthesis, and the production of collagen (Fig. 1D).
Reference: FEBS Open Bio. 2021 Aug; 11(8): 2340–2349. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8329776/
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMF |
14.0 |
43.92 |
| Ethanol |
16.0 |
50.20 |
| PBS (pH 7.2) |
0.5 |
1.57 |
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
318.75
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
1. Kikuchi R, Maeda Y, Tsuji T, Yamaguchi K, Abe S, Nakamura H, Aoshiba K. Fenofibrate inhibits TGF-β-induced myofibroblast differentiation and activation in human lung fibroblasts in vitro. FEBS Open Bio. 2021 Jul 6;11(8):2340–9. doi: 10.1002/2211-5463.13247. Epub ahead of print. PMID: 34228906; PMCID: PMC8329776.
2. Crakes KR, Pires J, Quach N, Ellis-Reis RE, Greathouse R, Chittum KA, Steiner JM, Pesavento P, Marks SL, Dandekar S, Gilor C. Fenofibrate promotes PPARα-targeted recovery of the intestinal epithelial barrier at the host-microbe interface in dogs with diabetes mellitus. Sci Rep. 2021 Jun 29;11(1):13454. doi: 10.1038/s41598-021-92966-7. PMID: 34188162; PMCID: PMC8241862.
3. Mandala A, Chen WJ, Armstrong A, Malhotra MR, Chavalmane S, McCommis KS, Chen A, Carpenter D, Biswas P, Gnana-Prakasam JP. PPARα Agonist Fenofibrate Attenuates Iron Induced Liver Injury in Mice by Modulating the Sirt3 and β-catenin Signaling. Am J Physiol Gastrointest Liver Physiol. 2021 Jul 21. doi: 10.1152/ajpgi.00129.2021. Epub ahead of print. PMID: 34287090.
4. Feng X, Gao X, Wang S, Huang M, Sun Z, Dong H, Yu H, Wang G. PPAR-α Agonist Fenofibrate Prevented Diabetic Nephropathy by Inhibiting M1 Macrophages via Improving Endothelial Cell Function in db/db Mice. Front Med (Lausanne). 2021 Jun 29;8:652558. doi: 10.3389/fmed.2021.652558. PMID: 34268320; PMCID: PMC8275839.
In vitro protocol:
1. Kikuchi R, Maeda Y, Tsuji T, Yamaguchi K, Abe S, Nakamura H, Aoshiba K. Fenofibrate inhibits TGF-β-induced myofibroblast differentiation and activation in human lung fibroblasts in vitro. FEBS Open Bio. 2021 Jul 6;11(8):2340–9. doi: 10.1002/2211-5463.13247. Epub ahead of print. PMID: 34228906; PMCID: PMC8329776.
2. Crakes KR, Pires J, Quach N, Ellis-Reis RE, Greathouse R, Chittum KA, Steiner JM, Pesavento P, Marks SL, Dandekar S, Gilor C. Fenofibrate promotes PPARα-targeted recovery of the intestinal epithelial barrier at the host-microbe interface in dogs with diabetes mellitus. Sci Rep. 2021 Jun 29;11(1):13454. doi: 10.1038/s41598-021-92966-7. PMID: 34188162; PMCID: PMC8241862.
In vivo protocol:
1. Mandala A, Chen WJ, Armstrong A, Malhotra MR, Chavalmane S, McCommis KS, Chen A, Carpenter D, Biswas P, Gnana-Prakasam JP. PPARα Agonist Fenofibrate Attenuates Iron Induced Liver Injury in Mice by Modulating the Sirt3 and β-catenin Signaling. Am J Physiol Gastrointest Liver Physiol. 2021 Jul 21. doi: 10.1152/ajpgi.00129.2021. Epub ahead of print. PMID: 34287090.
2. Feng X, Gao X, Wang S, Huang M, Sun Z, Dong H, Yu H, Wang G. PPAR-α Agonist Fenofibrate Prevented Diabetic Nephropathy by Inhibiting M1 Macrophages via Improving Endothelial Cell Function in db/db Mice. Front Med (Lausanne). 2021 Jun 29;8:652558. doi: 10.3389/fmed.2021.652558. PMID: 34268320; PMCID: PMC8275839.
1: Modjtahedi BS, Bose N, Papakostas TD, Morse L, Vavvas DG, Kishan AU. Lipids and Diabetic Retinopathy. Semin Ophthalmol. 2016;31(1-2):10-8. doi: 10.3109/08820538.2015.1114869. Review. PubMed PMID: 26959124.
2: Sando KR, Knight M. Nonstatin therapies for management of dyslipidemia: a review. Clin Ther. 2015 Oct 1;37(10):2153-79. doi: 10.1016/j.clinthera.2015.09.001. Epub 2015 Sep 26. Review. PubMed PMID: 26412799.
3: Ouwens MJ, Nauta J, Ansquer JC, Driessen S. Systematic literature review and meta-analysis of dual therapy with fenofibrate or fenofibric acid and a statin versus a double or equivalent dose of statin monotherapy. Curr Med Res Opin. 2015 Dec;31(12):2273-85. doi: 10.1185/03007995.2015.1098597. Epub 2015 Nov 5. Review. PubMed PMID: 26397380.
4: Zhang C, Wang H, Nie J, Wang F. Protective factors in diabetic retinopathy: focus on blood-retinal barrier. Discov Med. 2014 Sep;18(98):105-12. Review. PubMed PMID: 25227751.
5: Ling H, Luoma JT, Hilleman D. A Review of Currently Available Fenofibrate and Fenofibric Acid Formulations. Cardiol Res. 2013 Apr;4(2):47-55. doi: 10.4021/cr270w. Epub 2013 May 9. Review. PubMed PMID: 28352420; PubMed Central PMCID: PMC5358213.
6: Filippatos TD. A review of time courses and predictors of lipid changes with fenofibric acid-statin combination. Cardiovasc Drugs Ther. 2012 Jun;26(3):245-55. doi: 10.1007/s10557-012-6394-0. Review. PubMed PMID: 22592524; PubMed Central PMCID: PMC3368211.
7: Saurav A, Kaushik M, Mohiuddin SM. Fenofibric acid for hyperlipidemia. Expert Opin Pharmacother. 2012 Apr;13(5):717-22. doi: 10.1517/14656566.2012.658774. Epub 2012 Mar 9. Review. PubMed PMID: 22404421.
8: Campbell J, Mohiuddin SM. The role of a new formulation of fenofibric acid in the treatment of mixed dyslipidemia in type 2 diabetes. Drugs Today (Barc). 2010 Oct;46(10):757-64. doi: 10.1358/dot.2010.46.10.1519652. Review. PubMed PMID: 21076712.
9: Moutzouri E, Kei A, Elisaf MS, Milionis HJ. Management of dyslipidemias with fibrates, alone and in combination with statins: role of delayed-release fenofibric acid. Vasc Health Risk Manag. 2010 Aug 9;6:525-39. Review. PubMed PMID: 20730069; PubMed Central PMCID: PMC2922314.
10: Alagona P Jr. Fenofibric acid: a new fibrate approved for use in combination with statin for the treatment of mixed dyslipidemia. Vasc Health Risk Manag. 2010 May 25;6:351-62. Review. PubMed PMID: 20531954; PubMed Central PMCID: PMC2879297.
11: Joshi PH, Jacobson TA. Therapeutic options to further lower C-reactive protein for patients on statin treatment. Curr Atheroscler Rep. 2010 Jan;12(1):34-42. doi: 10.1007/s11883-009-0075-x. Review. PubMed PMID: 20425269.
12: Schima SM, Maciejewski SR, Hilleman DE, Williams MA, Mohiuddin SM. Fibrate therapy in the management of dyslipidemias, alone and in combination with statins: role of delayed-release fenofibric acid. Expert Opin Pharmacother. 2010 Apr;11(5):731-8. doi: 10.1517/14656560903575639. Review. PubMed PMID: 20210682.
13: Adeghate E, Kalasz H, Veress G, Teke K. Medicinal chemistry of drugs used in diabetic cardiomyopathy. Curr Med Chem. 2010;17(6):517-51. Review. PubMed PMID: 20015035.
14: Garg R, Angus E, Fincher S. Capecitabine-induced severe hypertriglyceridaemia and diabetes: a case report and review of the literature. Diabet Med. 2009 Dec;26(12):1308-9. doi: 10.1111/j.1464-5491.2009.02842.x. Review. PubMed PMID: 20002489.
15: Jacobson TA. Myopathy with statin-fibrate combination therapy: clinical considerations. Nat Rev Endocrinol. 2009 Sep;5(9):507-18. doi: 10.1038/nrendo.2009.151. Epub 2009 Jul 28. Review. PubMed PMID: 19636324.
16: Alagona P Jr. Beyond LDL cholesterol: the role of elevated triglycerides and low HDL cholesterol in residual CVD risk remaining after statin therapy. Am J Manag Care. 2009 Mar;15(3 Suppl):S65-73. Review. PubMed PMID: 19355805.
17: Filippatos T, Milionis HJ. Treatment of hyperlipidaemia with fenofibrate and related fibrates. Expert Opin Investig Drugs. 2008 Oct;17(10):1599-614. doi: 10.1517/13543784.17.10.1599 . Review. PubMed PMID: 18808320.
18: Hernando MD, Agüera A, Fernández-Alba AR. LC-MS analysis and environmental risk of lipid regulators. Anal Bioanal Chem. 2007 Feb;387(4):1269-85. Epub 2006 Sep 20. Review. PubMed PMID: 17047939.
19: Wierzbicki AS, Mikhailidis DP, Wray R. Drug treatment of combined hyperlipidemia. Am J Cardiovasc Drugs. 2001;1(5):327-36. Review. PubMed PMID: 14728015.
20: Sharpe M, Ormrod D, Jarvis B. Micronized fenofibrate in dyslipidemia: a focus on plasma high-density lipoprotein cholesterol (HDL-C) levels. Am J Cardiovasc Drugs. 2002;2(2):125-32; discussion 133-4. Review. PubMed PMID: 14727988.
