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  3. Fenofibrate

Fenofibrate (GMP) 是 GMP 级别的 Fenofibrate (HY-17356)。GMP 级别的小分子可用做细胞疗法中的辅助试剂。Fenofibrate 是一种选择性的 PPARα 激动剂,EC50 为 30 μM。Fenofibrate 抑制细胞色素 P450 亚型,对 CYP2C19CYP2B6CYP2C9CYP2C8CYP3A4IC50 分别为 0.2,0.7,9.7,4.8 和 142.1 μM。

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Fenofibrate

Fenofibrate Chemical Structure

CAS No. : 49562-28-9

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Fenofibrate 的其他形式现货产品:

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Other Forms of Fenofibrate:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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.

细胞效力
(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]
体外研究
(In Vitro)

Fenofibrate 是一种相对有效的 CYP2B6 (IC50=0.7±0.2 μM) 和 CYP2C19 (IC50=0.2±0.1 μM) 抑制剂。Fenofibrate 也是 CYP2C8 (IC50=4.8±1.7 μM) 和 CYP2C9 (IC50=9.7 μM) 的中度抑制剂[1]
Fenofibrate 以比 PPARα 更高的亲和力结合并抑制细胞色素 P450 环氧化酶 (CYP)2C。Fenofibrate 是一种众所周知的 PPARα 激动剂,但对 209 种常用处方药和相关异生素的体外评估表明,Fenofibrate 也是细胞色素 P450 环氧化酶 (CYP)2C 的有效抑制剂。Fenofibrate 对 CYP2C 的亲和力 (EC50=2.39±0.4 μM) 比对 PPARα (EC50=30 μM) 高 10 倍以上。
低剂量的 Fenofibrate 可抑制 CYP2C8 活性,而不激活 PPARα[2]。 Fenofibrate (25 μM, 24小时) 降低 GSC 侵袭和 GSC 干细胞标记物 (CD133, Oct4) 的表达[3]
Fenofibrate (5 μM, 7 天) 能抑制线粒体诱导的 DMD hiPSC 衍生心肌细胞凋亡[4]
Fenofibrate (25 μM, 72 小时) 不能提高患者 iPSC 衍生神经祖细胞中 TPP1 的活性[5]

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

体内研究
(In Vivo)

每日摄入如此低剂量(10 μg/g/天)的 Fenofibrate 可抑制 CYP2C8 过表达诱导的视网膜和脉络膜新生血管形成,抑制率分别为 29% (P=0.021) 和 36% (P=1.2×10-9)[2]

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

Clinical Trial
分子量

360.83

Formula

C20H21ClO4

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    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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产品名称:
Fenofibrate
目录号:
HY-17356G
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