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Fenofibric acid (FNF acid) 是 fenofibrate 的活性代谢物,是PPAR 激动剂,对 PPARα、PPARγ 和 PPARδ 的EC50值分别为 22.4、1.47 和 1.06 µM。它抑制COX-2的活性,IC50值为 48 nM。
Fenofibric acid (FNF acid) 是 fenofibrate 的活性代谢物,是PPAR 激动剂,对 PPARα、PPARγ 和 PPARδ 的EC50值分别为 22.4、1.47 和 1.06 µM。它抑制COX-2的活性,IC50值为 48 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 g | ¥ 331 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 274 | 现货 |
产品描述 | Fenofibric acid (FNF acid) is the active form of fenofibrate, a synthetic phenoxy-isobutyric acid derivate with antihyperlipidemic activity. |
靶点活性 | PPARα:22.4 µM(EC50), PPARδ:1.06 µM(EC50), PPARγ:1.47 µM(EC50), COX-2:48 nM |
体外活性 | 纤维酸是纤维酸药物的有效形式,也是过氧化物酶体增殖剂激活受体-α(PPARα)的激活剂,已知具有提高高密度脂蛋白(HDL)的效果。纤维酸通过增强脂肪酸的分解作用,相应降低血浆脂质水平,主要是甘油三酯(TG)。Fenofibric acid 增加ABCA1的表达和apoA-I介导的HDL产生。ABCA1表达的增强通过增加ABCA1基因的转录而产生,这一过程依赖于LXR[1]。 |
体内活性 | Fenofibric acid 降低OIR小鼠体内循环EPC(内皮祖细胞)的异常增加。Fenofibric acid对OIR模型中EPC动员的抑制作用依赖于PPARα。Fenofibric acid 以PPARα依赖的方式抑制低氧诱导的视网膜EPC增加Fenofibric acid 减少循环中CXCR4阳性EPC的数量,下调血清SDF-1水平,并抑制视网膜中HIF-1a与SDF-1的过表达[1]。 |
细胞实验 | PPAR activators fenofibric acid is dissolved in DMSO and added to the culture medium containing 0.2% BSA. RAW264 cells are washed with PBS and cultured an additional 48 hours in the presence of fenofibric acid in DMEM/F-12(1:1) medium containing 2% TCM and 0.2% BSA. During the last 24 hours of the drug treatment, 300 mol/L of dibutyryl cAMP and apoA-I (10 μg/mL) are added to the medium. THP-1 cells are also treated with the compound and apoA-I in 0.2% BSA-RPMI 1640 medium and 0.1% BSA-MEM. Cholesterol and choline-phospholipid released into the medium by apoA-I are determined enzymatically. Adherent cells are dissolved in 0.1 N NaOH for protein determination by bicinchoninic acid protein assay system. (Only for Reference) |
别名 | 非诺贝特酸, Trilipix, NSC 281318, FNF acid |
分子量 | 318.75 |
分子式 | C17H15ClO4 |
CAS No. | 42017-89-0 |
Smiles | C(=O)(C1=CC=C(OC(C(O)=O)(C)C)C=C1)C2=CC=C(Cl)C=C2 |
密度 | 1.286 g/cm3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 60 mg/mL (188.24 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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