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  3. Fenofibrate

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.

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Fenofibrate

Fenofibrate Chemical Structure

CAS No. : 49562-28-9

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Description

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.

Cellular Effect
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
[PMID: 12904063]
CHO-K1 EC50
50 μM
Compound: Fenofibrate
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
[PMID: 12904063]
COS-1 EC50
2000 nM
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
[PMID: 19530681]
COS-1 EC50
> 5000 nM
Compound: Fenofibrate
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
[PMID: 19530681]
HEK293 EC50
33.51 μM
Compound: Fenofibrate
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
[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
[PMID: 31320147]
LoVo IC50
13.2 μM
Compound: 24
Antiproliferative activity against human LoVo cells after 120 hrs by MTT assay
Antiproliferative activity against human LoVo cells after 120 hrs by MTT assay
[PMID: 16680159]
MIA PaCa-2 IC50
8.4 μM
Compound: 24
Antiproliferative activity against human MIAPaCa2cells after 120 hrs by MTT assay
Antiproliferative activity against human MIAPaCa2cells after 120 hrs by MTT assay
[PMID: 16680159]
PC-3 IC50
18 μM
Compound: 24
Antiproliferative activity against human PC3 cells after 120 hrs by MTT assay
Antiproliferative activity against human PC3 cells after 120 hrs by MTT assay
[PMID: 16680159]
U-87MG ATCC IC50
74.5 μM
Compound: 24
Antiproliferative activity against human U87MG cells after 120 hrs by MTT assay
Antiproliferative activity against human U87MG cells after 120 hrs by MTT assay
[PMID: 16680159]
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].
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.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

360.83

Formula

C20H21ClO4

CAS No.
SMILES

CC(C)(OC1=CC=C(C(C2=CC=C(Cl)C=C2)=O)C=C1)C(OC(C)C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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