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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 49562-28-9
- 分子式: C20H21ClO4
- 分子量:360.83
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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HY-17356
Fenofibrate -
HY-17356R
Fenofibrate (Standard) -
HY-B0258
GemfibrozilCytochrome P450 Inhibitor -
HY-50935
TroglitazonePPARγ Agonist -
HY-13956
PioglitazonePPARγ Agonist -
HY-17386
RosiglitazonePPARγ Agonist -
HY-B0258R
Gemfibrozil (Standard) -
HY-10838
GW 501516PPARδ Agonist -
HY-16578
GW9662PPARγ Antagonist -
HY-B0287
ClofibratePPAR Agonist -
HY-16995
Pirinixic acidPPAR Agonist -
HY-13861
GW7647PPAR Agonist
生物活性
製品説明
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
15.9 μM
Compound: 24
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Antiproliferative activity against human A549 cells after 120 hrs by MTT assay
Antiproliferative activity against human A549 cells after 120 hrs by MTT assay
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[PMID: 16680159] |
| CHO-K1 | EC50 |
49 μM
Compound: Fenofibrate
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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
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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
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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] |
体外実験
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.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 49562-28-9
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分子量 360.83
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Fenofibrate (GMP) 関連分類
HY-17356G 関連分類
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