Fenofibrate
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MedKoo CAT#: 317866

CAS#: 49562-28-9

Description: Fenofibrate (INN) is a drug of the fibrate class. It is mainly used to reduce cholesterol levels in patients at risk of cardiovascular disease. Like other fibrates, it reduces both low-density lipoprotein (LDL) and very low density lipoprotein (VLDL) levels, as well as increasing high-density lipoprotein (HDL) levels and reducing triglyceride levels. It is used alone or along with statins in the treatment of hypercholesterolemia and hypertriglyceridemia. Fenofibrate has been used since 1975, is one of the most commonly prescribed fibrates, and has a well known efficacy and tolerability profile.


Chemical Structure

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Fenofibrate
CAS# 49562-28-9

Theoretical Analysis

MedKoo Cat#: 317866
Name: Fenofibrate
CAS#: 49562-28-9
Chemical Formula: C20H21ClO4
Exact Mass: 360.11
Molecular Weight: 360.831
Elemental Analysis: C, 66.57; H, 5.87; Cl, 9.83; O, 17.74

Price and Availability

Size Price Availability Quantity
1g USD 150 Ready to ship
2g USD 250 Ready to ship
5g USD 450 Ready to ship
10g USD 750 Ready to ship
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Synonym: Fenofibrate, Tricor, Procetofen, Controlip, Durafenat, LF 178, LF178, LF-178, Lipanthyl, Normalip, Secalip

IUPAC/Chemical Name: propan-2-yl 2-[4-(4-chlorobenzoyl)phenoxy]-2-methylpropanoate

InChi Key: YMTINGFKWWXKFG-UHFFFAOYSA-N

InChi Code: InChI=1S/C20H21ClO4/c1-13(2)24-19(23)20(3,4)25-17-11-7-15(8-12-17)18(22)14-5-9-16(21)10-6-14/h5-13H,1-4H3

SMILES Code: CC(C)(OC1=CC=C(C(C2=CC=C(Cl)C=C2)=O)C=C1)C(OC(C)C)=O

Appearance: White to off-white solid powder.

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, not in water

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

More Info:

Product Data:
Safety Data Sheet (SDS):
Biological target: Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
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: Intrinsically, PPARα KO mice showed significant downregulation of hepatic Sirt3 levels. In addition, treatment of iron overload mice with PPARα agonist fenofibrate reduced hepatic iron accumulation and prevented iron induced downregulation of liver Sirt3 and active β-catenin, mitigating the progression of fibrosis. Reference: Am J Physiol Gastrointest Liver Physiol. 2021 Jul 21. https://pubmed.ncbi.nlm.nih.gov/34287090/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMF 30.0 83.14
DMF:PBS (pH 7.2) (1:3) 0.3 0.00
Ethanol 36.4 100.77

Preparing Stock Solutions

The following data is based on the product molecular weight 360.83 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.

Recalculate based on batch purity %
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.

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1: Derosa G, Maffioli P, Sahebkar A. Plasma uric acid concentrations are reduced by fenofibrate: A systematic review and meta-analysis of randomized placebo-controlled trials. Pharmacol Res. 2015 Dec;102:63-70. doi: 10.1016/j.phrs.2015.09.012. Epub 2015 Sep 15. Review. PubMed PMID: 26384444.

2: Zhang Y, Li S, He L, Wang F, Chen K, Li J, Liu T, Zheng Y, Wang J, Lu W, Zhou Y, Yin Q, Xia Y, Zhou Y, Lu J, Guo C. Combination therapy of fenofibrate and ursodeoxycholic acid in patients with primary biliary cirrhosis who respond incompletely to UDCA monotherapy: a meta-analysis. Drug Des Devel Ther. 2015 May 25;9:2757-66. doi: 10.2147/DDDT.S79837. eCollection 2015. Review. PubMed PMID: 26045661; PubMed Central PMCID: PMC4448927.

3: Simó R, Simó-Servat O, Hernández C. Is fenofibrate a reasonable treatment for diabetic microvascular disease? Curr Diab Rep. 2015 May;15(5):24. doi: 10.1007/s11892-015-0599-0. Review. PubMed PMID: 25772642.

4: Schofield JD, Liu Y, France MW, Sandle L, Soran H. A review of paradoxical HDL-C responses to fenofibrate, illustrated by a case report. J Clin Lipidol. 2014 Jul-Aug;8(4):455-9. doi: 10.1016/j.jacl.2014.05.003. Epub 2014 Jun 6. Review. PubMed PMID: 25110229.

5: Hernández Mijares A. [Combination of pravastatin and fenofibrate (Pravafenix ®). Safety studies]. Clin Investig Arterioscler. 2014 Jul;26 Suppl 1:25-30. doi: 10.1016/S0214-9168(14)70023-3. Review. Spanish. PubMed PMID: 25043544.

6: Noonan JE, Jenkins AJ, Ma JX, Keech AC, Wang JJ, Lamoureux EL. An update on the molecular actions of fenofibrate and its clinical effects on diabetic retinopathy and other microvascular end points in patients with diabetes. Diabetes. 2013 Dec;62(12):3968-75. doi: 10.2337/db13-0800. Review. PubMed PMID: 24264394; PubMed Central PMCID: PMC3837039.

7: Kostapanos MS, Kei A, Elisaf MS. Current role of fenofibrate in the prevention and management of non-alcoholic fatty liver disease. World J Hepatol. 2013 Sep 27;5(9):470-8. doi: 10.4254/wjh.v5.i9.470. Review. PubMed PMID: 24073298; PubMed Central PMCID: PMC3782684.

8: Attridge RL, Frei CR, Ryan L, Koeller J, Linn WD. Fenofibrate-associated nephrotoxicity: a review of current evidence. Am J Health Syst Pharm. 2013 Jul 15;70(14):1219-25. doi: 10.2146/ajhp120131. Review. PubMed PMID: 23820458.

9: Simó R, Roy S, Behar-Cohen F, Keech A, Mitchell P, Wong TY. Fenofibrate: a new treatment for diabetic retinopathy. Molecular mechanisms and future perspectives. Curr Med Chem. 2013;20(26):3258-66. Review. PubMed PMID: 23745548.

10: Kostapanos MS, Florentin M, Elisaf MS. Fenofibrate and the kidney: an overview. Eur J Clin Invest. 2013 May;43(5):522-31. doi: 10.1111/eci.12068. Epub 2013 Mar 11. Review. PubMed PMID: 23480615.

11: Guo J, Meng F, Ma N, Li C, Ding Z, Wang H, Hou R, Qin Y. Meta-analysis of safety of the coadministration of statin with fenofibrate in patients with combined hyperlipidemia. Am J Cardiol. 2012 Nov 1;110(9):1296-301. doi: 10.1016/j.amjcard.2012.06.050. Epub 2012 Jul 27. Review. PubMed PMID: 22840347.

12: Wong TY, Simó R, Mitchell P. Fenofibrate - a potential systemic treatment for diabetic retinopathy? Am J Ophthalmol. 2012 Jul;154(1):6-12. doi: 10.1016/j.ajo.2012.03.013. Review. PubMed PMID: 22709833.

13: Farnier M. Pravastatin and fenofibrate in combination (Pravafenix(®)) for the treatment of high-risk patients with mixed hyperlipidemia. Expert Rev Cardiovasc Ther. 2012 May;10(5):565-75. doi: 10.1586/erc.12.37. Review. Erratum in: Expert Rev Cardiovasc Ther. 2013 Feb;11(2):253-4. PubMed PMID: 22651832.

14: Elijah IE, Børsheim E, Maybauer DM, Finnerty CC, Herndon DN, Maybauer MO. Role of the PPAR-α agonist fenofibrate in severe pediatric burn. Burns. 2012 Jun;38(4):481-6. doi: 10.1016/j.burns.2011.12.004. Epub 2012 Jan 9. Review. PubMed PMID: 22226866; PubMed Central PMCID: PMC3669757.

15: Susekov AV, Khokhlova NV. [Perspectives of the use of fenofibrate in patients with type 2 diabetes mellitus: what is new after the ACCORD Study?]. Kardiologiia. 2011;51(9):68-74. Review. Russian. PubMed PMID: 21943011.

16: McKeage K, Keating GM. Fenofibrate: a review of its use in dyslipidaemia. Drugs. 2011 Oct 1;71(14):1917-46. doi: 10.2165/11208090-000000000-00000. Review. PubMed PMID: 21942979.

17: Simó R, Hernández C. Prevention and treatment of diabetic retinopathy: evidence from large, randomized trials. The emerging role of fenofibrate. Rev Recent Clin Trials. 2012 Feb;7(1):71-80. Review. PubMed PMID: 21864248.

18: Filippatos TD, Elisaf MS. Fenofibrate plus simvastatin (fixed-dose combination) for the treatment of dyslipidaemia. Expert Opin Pharmacother. 2011 Aug;12(12):1945-58. doi: 10.1517/14656566.2011.593509. Epub 2011 Jul 8. Review. PubMed PMID: 21736529.

19: Keating GM. Fenofibrate: a review of its lipid-modifying effects in dyslipidemia and its vascular effects in type 2 diabetes mellitus. Am J Cardiovasc Drugs. 2011 Aug 1;11(4):227-47. doi: 10.2165/11207690-000000000-00000. Review. PubMed PMID: 21675801.

20: Hermans MP. Non-invited review: prevention of microvascular diabetic complications by fenofibrate: lessons from FIELD and ACCORD. Diab Vasc Dis Res. 2011 Jul;8(3):180-9. doi: 10.1177/1479164111407783. Epub 2011 May 16. Review. PubMed PMID: 21576195.