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My CartCAS：49562-28-9
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥99%
Appearance：White to off-white Solid
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| CAS | 49562-28-9 |
| Name | Fenofibrate |
| Molecular Formula | C20H21ClO4 |
| Molecular Weight | 360.83 |
| Solubility | Soluble in DMSO ≥3.6mg/mL |
| Purity | ≥99% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 256-376-3 |
| MDL | MFCD00133314 |
| SMILES | CC(C)(OC1=CC=C(C(C2=CC=C(Cl)C=C2)=O)C=C1)C(OC(C)C)=O |
| InChIKey | YMTINGFKWWXKFG-UHFFFAOYSA-N |
| InChI | InChI=1S/C20H21ClO4/c1-13(2)24-19(23)20(3,4)25-17-11-7-15(8-12-17)18(22)14-5-9-16(21)10-6-14/h5-13H,1-4H3 |
| PubChem CID | 3339 |
| Target Point | PPAR;Cytochrome P450 |
| Passage | Cell Cycle;DNA Damage/DNA Repair;Metabolic Enzyme&Protease |
| Background | Fenofibrate is a selective PPARα agonist. Fenofibrate inhibits cytochrome P450 isoforms such as CYP2C19, CYP2B6, CYP2C9, CYP2C8 and CYP3A4. |
| Biological Activity | Fenofibrate是 PPARα 激动剂，EC50 为30 μM。[1-2] |
| IC50 | CYP2C19:0.2μM;CYP2B6:0.7μM [1] |
| In Vitro | 非诺贝特是一种相对有效的CYP2B6抑制剂(IC50 = 0.7±0.2μM)和CYP2C19(IC50 = 0.2±0.1μM)。非诺贝特也是CYP2C8的中度抑制剂(IC50 = 4.8±1.7μM)和CYP2C9(IC50 =9.7μM)[1]。非诺贝特以高于PPARα的亲和力结合并抑制细胞色素P450环加氧酶(CYP)2C。非诺贝特是一种众所周知的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，非诺贝特也是细胞色素P450环氧化酶(CYP)2C的有效抑制剂。非诺贝特对CYP2C的亲和力比对PPARα(EC50 =30μM)高> 10倍(EC50 = 2.39±0.4μM)。低剂量的非诺贝特抑制CYP2C8活性而不激活PPARα[2]。 |
| In Vivo | 在这种低剂量(10μg/ g /天)下每日摄入非诺贝特可抑制由CYP2C8过度表达诱导的视网膜和脉络膜新生血管形成，分别为29％(P = 0.021)和36％(P = 1.2×10-9)[2]。 |
| Animal Experiment | 小鼠[2]使用小鼠氧诱导的视网膜病变(OIR)模型。简言之，为了诱导视网膜新生血管形成，小鼠幼仔及其哺乳母亲暴露于从P7到P12的75±3％氧气。用于较高剂量的非诺贝特(F6020)治疗(100mg/kg /天)。将非诺贝特溶解在玉米油中以制备100mg/mL溶液，并将纯玉米油用作媒介物对照。对于较低剂量的治疗(10mg/kg /天)，将非诺贝特溶解在10％DMSO，D2650中以制备10mg/mL溶液，并使用10％DMSO作为媒介物对照。回到室内空气后，每天从P12到P16口服强抗诺非贝特(100或10mg/kg)或载体对照。在P17，在安乐死后立即摘出眼，并在室温下在PBS中的4％多聚甲醛中固定1小时。然后解剖视网膜并在室温下用Alexa Fluor 594缀合的同工凝集素GS-IB4(10μg/ mL)染色过夜。用PBS洗涤后，将视网膜安装到显微镜载玻片上，感光体侧朝下并嵌入SlowFade抗褪色封固剂中。 |
| Kinase Experiment | 非诺贝特，他汀类药物(阿托伐他汀，洛伐他汀，普伐他汀，辛伐他汀和辛伐他汀酸，辛伐他汀的活性形式)和格列吡嗪对重组人CYP1A2，CYP2B6，CYP2C8，CYP2C9，CYP2C19，CYP2D6和CYP3A4的半数抑制浓度(IC50s)使用荧光CYP450抑制测定法测定。简而言之，将药物溶解在甲醇或乙腈中。在96孔测定板中，将药物在含有辅因子的溶液中稀释至一系列浓度，所述辅因子包括NADP +(终浓度1.3mM)，MgCl 2(终浓度3.3m M)，葡萄糖-6-磷酸(G6P，终浓度3.3mM)。)和葡萄糖-6-磷酸脱氢酶(终浓度0.4U/mL)。将混合物在37℃下预温育10分钟。将酶和荧光底物在磷酸钠反应缓冲液(pH 7.4，终浓度200mM)中稀释至所需浓度并混合。通过将酶和底物混合物添加到辅因子和药物混合物中来开始反应。所有测定的最终反应体积为200μL。在37℃下孵育预定的时间段(15至45分钟)后，通过添加75μL猝灭溶液(0.5M Tris碱或2N NaOH)终止反应。使用BioTek Synergy 2荧光读数器测定荧光。每种药物以八种浓度一式两份进行测试。为了估计IC 50，使用针对背景校正的净荧光计算抑制百分比。然后将抑制百分比的值拟合到三或四参数对数逻辑模型[1]。 |
| Data Literature Source | [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. [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. |
| Unit | Bottle |
| Specification | 100mg 10mM*1mL in DMSO 500mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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