Tricor, Procetofen, LF-178, Lipanthyl, Normalip, Secalip; Fenofibrate; LF 178, LF178,Controlip, durafenat
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| 5g |
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| 25g |
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Purity: ≥98%
Fenofibrate (Tricor, Procetofen, LF-178, Lipanthyl, NSC-281319; Controlip, Normalip, Secalip, durafenat, Trilipix) is a fibric acid based anti-hyperlipidemic drug of the fibrate class approved for clinical uses as a lipid-lowering agent. Fenofibrate acts as selective PPARα agonist with an EC50 of 30 μM. It is used to reduce cholesterol levels in patients at risk of cardiovascular disease.
| ln Vitro |
Fenofibrate inhibits CYP2B6 (IC50=0.7±0.2 μM) and CYP2C19 (IC50=0.2±0.1 μM) with a fair degree of potency. According to reference [1], fenofibrate exhibits moderate inhibitory effects on CYP2C8 (IC50=4.8±1.7 μM) and CYP2C9 (IC50=9.7 μM). Compared to PPARα, fenofibrate has a greater affinity for cytochrome P450 epoxygenase (CYP)2C and inhibits it. Fenofibrate is a well-known PPARα agonist, but it also appears to be a strong inhibitor of cytochrome P450 epoxygenase (CYP)2C, according to an in vitro evaluation of 209 commonly given medications and related xenobiotics. Fenofibrate has >10 times the affinity for CYP2C (EC50=2.39±0.4 μM) compared to PPARα (EC50=30 μM). Low doses of fenofibrate reduce CYP2C8 activity without activating PPARα[2].
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| ln Vivo |
At a modest dose of 10 μg/g/day, fenofibrate suppresses CYP2C8 overexpression-induced retinal and choroidal neovascularization by 29% (P=0.021) and 36% (P=1.2×10−9), respectively, on a daily basis[2].
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| References |
[1]. Schelleman H, et al. Pharmacoepidemiologic and in vitro evaluation of potential drug-drug interactions of sulfonylureas with fibrates and statins. Br J Clin Pharmacol. 2014 Sep;78(3):639-48.
[2]. Gong Y, et al. Fenofibrate Inhibits Cytochrome P450 Epoxygenase 2C Activity to Suppress Pathological Ocular Angiogenesis. EBioMedicine. 2016 Sep 30. pii: S2352-3964(16)30448-0 |
| Molecular Formula |
C20H21CLO4
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| Molecular Weight |
360.83
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| CAS # |
49562-28-9
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| Related CAS # |
Fenofibrate (Standard);49562-28-9;Fenofibrate;49562-28-9;Fenofibrate-d6;1092484-56-4;Fenofibrate-d4;1092484-57-5
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| SMILES |
ClC1C([H])=C([H])C(=C([H])C=1[H])C(C1C([H])=C([H])C(=C([H])C=1[H])OC(C(=O)OC([H])(C([H])([H])[H])C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H])=O
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| InChi Key |
YMTINGFKWWXKFG-UHFFFAOYSA-N
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| 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
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| Chemical Name |
propan-2-yl 2-[4-(4-chlorobenzoyl)phenoxy]-2-methylpropanoate
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.93 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (6.93 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.93 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 33.33 mg/mL (92.37 mM) in Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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