非诺贝特酸 T1402

Product Introduction
Bioactivity


英文名: Fenofibric acid

描述: 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。

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)

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]。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 60 mg/mL (188.24 mM)


关键字: Peroxisome proliferator-activated receptors | Inhibitor | COX | Fenofibric acid | inhibit | NSC-281318 | Cyclooxygenase | PPAR | NSC281318

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相关库: Drug Repurposing Compound Library | Bioactive Lipid Compound Library | Pyroptosis Compound Library | Drug-induced Liver Injury (DILI) Compound Library | Anti-Cancer Drug Library | Endoplasmic Reticulum Stress Compound Library | Pediatric Drug Library | Anti-Cancer Approved Drug Library | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途