Fenofibrate (GMP) is Fenofibrate (HY-17356) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. 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.
For research use only. We do not sell to patients.
- CAS No.: 49562-28-9
- Formula: C20H21ClO4
- Molecular Weight:360.83
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
15.9 μM
Compound: 24
|
Antiproliferative activity against human A549 cells after 120 hrs by MTT assay
Antiproliferative activity against human A549 cells after 120 hrs by MTT assay
|
[PMID: 16680159] |
| CHO-K1 | EC50 |
49 μM
Compound: Fenofibrate
|
In vitro effective concentration for agonist activity on rat Peroxisome proliferator activated receptor alpha-Gal4 chimeric receptor in transfected CHO-K1 cells
In vitro effective concentration for agonist activity on rat Peroxisome proliferator activated receptor alpha-Gal4 chimeric receptor in transfected CHO-K1 cells
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[PMID: 12904063] |
| CHO-K1 | EC50 |
50 μM
Compound: Fenofibrate
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In vitro effective concentration for agonist activity on dog Peroxisome proliferator activated receptor alpha-Gal4 chimeric receptor in transfected CHO-K1 cells
In vitro effective concentration for agonist activity on dog Peroxisome proliferator activated receptor alpha-Gal4 chimeric receptor in transfected CHO-K1 cells
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[PMID: 12904063] |
| COS-1 | EC50 |
>5000 nM
Compound: Fenofibrate
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Agonist activity at human PPARgamma receptor expressed in african green monkey COS1 cells co-transfected with fused yeast Gal4-DBD by transactivation assay
Agonist activity at human PPARgamma receptor expressed in african green monkey COS1 cells co-transfected with fused yeast Gal4-DBD by transactivation assay
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[PMID: 19530681] |
| COS-1 | EC50 |
2 μM
Compound: Fenofibrate
|
Agonist activity at human PPARalpha receptor expressed in african green monkey COS1 cells co-transfected with fused yeast Gal4-DBD by transactivation assay
Agonist activity at human PPARalpha receptor expressed in african green monkey COS1 cells co-transfected with fused yeast Gal4-DBD by transactivation assay
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[PMID: 19530681] |
| HEK293 | EC50 |
33.51 μM
Compound: Fenofibrate
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Agonist activity at human PPARalpha expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay
Agonist activity at human PPARalpha expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay
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[PMID: 23265844] |
| HepG2 | EC50 |
50 μM
Compound: 1
|
Transactivation of human GAL4-fused PPARalpha LBD expressed in human HepG2 cells after 24 hrs by renilla luciferase reporter gene assay
Transactivation of human GAL4-fused PPARalpha LBD expressed in human HepG2 cells after 24 hrs by renilla luciferase reporter gene assay
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[PMID: 31320147] |
| LoVo | IC50 |
13.2 μM
Compound: 24
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Antiproliferative activity against human LoVo cells after 120 hrs by MTT assay
Antiproliferative activity against human LoVo cells after 120 hrs by MTT assay
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[PMID: 16680159] |
| MIA PaCa-2 | IC50 |
8.4 μM
Compound: 24
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Antiproliferative activity against human MIAPaCa2cells after 120 hrs by MTT assay
Antiproliferative activity against human MIAPaCa2cells after 120 hrs by MTT assay
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[PMID: 16680159] |
| PC-3 | IC50 |
18 μM
Compound: 24
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Antiproliferative activity against human PC3 cells after 120 hrs by MTT assay
Antiproliferative activity against human PC3 cells after 120 hrs by MTT assay
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[PMID: 16680159] |
| U-87MG ATCC | IC50 |
74.5 μM
Compound: 24
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Antiproliferative activity against human U87MG cells after 120 hrs by MTT assay
Antiproliferative activity against human U87MG cells after 120 hrs by MTT assay
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[PMID: 16680159] |
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].
Fenofibrate (25 μM, 24 h) decreases both GSC invasion and GSC expression of stem-cell markers (CD133, Oct4)[3].
Fenofibrate (5 μM, 7 d) can inhibit mitochondrion-induced apoptosis in DMD hiPSC-derived cardiomyocytes[4].
Fenofibrate (25 μM, 72 h) fail to increase tripeptidyl peptidase-1 (TPP1) activity in patient iPSC-derived neural progenitor cells[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 49562-28-9
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Molecular Weight 360.83
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Formula C20H21ClO4
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SMILES
CC(C)(OC1=CC=C(C(C2=CC=C(Cl)C=C2)=O)C=C1)C(OC(C)C)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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. [Content Brief]
[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. [Content Brief]
[3]. Binello E, et al. Characterization of fenofibrate-mediated anti-proliferative pro-apoptotic effects on high-grade gliomas and anti-invasive effects on glioma stem cells. J Neurooncol. 2014 Apr;117(2):225-34./ [Content Brief]
[4]. Sun C, et al. Duchenne muscular dystrophy hiPSC-derived myoblast drug screen identifies compounds that ameliorate disease in mdx mice. JCI Insight. 2020 Jun 4;5(11):e134287. [Content Brief]
[5]. Lojewski X, et al. Human iPSC models of neuronal ceroid lipofuscinosis capture distinct effects of TPP1 and CLN3 mutations on the endocytic pathway. Hum Mol Genet. 2014 Apr 15;23(8):2005-22. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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