Fenofibrate
产品说明书
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同义名 : | NSC-281319 |
| CAS号 : | 49562-28-9 | |
| 货号 : | A763996 | |
| 分子式 : | C20H21ClO4 | |
| 纯度 : | 97% | |
| 分子量 : | 360.83 | |
| MDL号 : | MFCD00133314 | |
| 存储条件： |
Pure form Sealed in dry,Room Temperature In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 105 mg/mL(290.99 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
2% DMSO+40% PEG 300+2% Tween 80+water 10 mg/mL |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, these enzymes are involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Peroxisome proliferator-activated receptors (PPARs) belong to the steroid hormone receptor superfamily. PPARs mediate the action of peroxisome proliferators, and affect the expression of target genes involved in cell proliferation, cell differentiation and in immune and inflammation responses. Fenofibrate is a PPARα agonist, and also a Cytochrome P450 Epoxygenase 2C (CYP2C) inhibitor. In vitro assessment revealed that the EC50 of Fenofibrate to CYP2C was 2.39±0.4 μM, while the EC50 of Fenofibrate to PPARα was 30 μM, suggesting higher affinity to CYP2C[3]. Based on fluorometric CYP450 inhibition assays, Fenofibrate also inhibited CYP2C19, CYP2C8 and CYP2C9 with the IC50s of 0.2 μM, 4.8 μM and 9.7 μM, respectively[4]. In animal experiments, Fenofibrate was administrated at the dose of 150 mg/kg orally in C57BL/6J (B6) or B6 × 129S4 mice for 8 days in the studies of withdrawal, loss of righting reflex, startle reflex, response to novelty, and EtOH clearance, and for the duration of the experiment in the studies of conditioned place preference and conditioned taste aversion. The results revealed that Fenofibrate decreased the novelty response, increased acute EtOH withdrawal severity, and increased EtOH-induced conditioned taste aversion， while EtOH-induced conditioned place preference was not altered. EtOH clearance was increased by fenofibrate. Response to novelty, acute withdrawal, and EtOH clearance show sex differences and could contribute to the reduced EtOH consumption following fenofibrate administration[5]. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT00673881 | Dyslipidemia | Phase 1 Phase 2 | Completed | - | United States, Illinois ... 展开 >> Radiant Research, 515 N State St, #2700 Chicago, Illinois, United States, 60610 收起 << |
| NCT00261352 | Type 2 Diabetes | Phase 3 | Terminated(The development pro... 展开 >>gram has been terminated) 收起 << | - | - |
| NCT00195793 | Hyperlipidemia | Phase 3 | Completed | - | - |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.77mL 0.55mL 0.28mL |
13.86mL 2.77mL 1.39mL |
27.71mL 5.54mL 2.77mL |
| 参考文献 |
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