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Clofibrate

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Chemical Structure| 637-07-0 同义名 : 氯贝丁酯 ;ICI 28257;NSC 79389;Clofibratum;Clofibrato;Atromid-S;Ethyl clofibrate
CAS号 : 637-07-0
货号 : A533783
分子式 : C12H15ClO3
纯度 : 98%
分子量 : 242.699
MDL号 : MFCD00000615
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(432.64 mM)，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
动物实验配方：
生物活性
描述 Clofibrate, a fibric acid derivative, is a selective agonist of PPARα with EC50 of 50 µM. Clofibrate has been used to treat hyperlipoproteinemia type III and severe hypertriglyceridemia[3]. Clofibrate (0.5, 1, 2 mM) increases FABP1 expression in two fatty acid (FA)-treated rat hepatoma cells. Clofibrate lowers ROS levels after early treatment, much more than late treatment in FA-treated cells[4]. Moreover, clofibrate administration to 7 days MI-rats exerts an antioxidant, pro-vasodilator expression profile, and anti-fibrotic effect suggesting that PPARα activation can be considered a therapeutic target to improve cardiac condition posterior to ischemia[5]. Giving CF (0.5% Clofibrate) to pregnant mice programmed greater HFD(high-fat diet)-induced WAT (white adipose tissue) browning in subcutaneous, but not in visceral fat, in their male offspring at adulthood[6].
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
NCT03031821 Prostate Cancer ... 展开 >> Metabolic Syndrome 收起 << Phase 3 Not yet recruiting June 1, 2023 Canada, British Columbia ... 展开 >> BC Cancer Agency - Vancouver Cancer Centre Not yet recruiting Vancouver, British Columbia, Canada, V5Z 4E6 Contact: Bernie Eigl, MD    604-877-6000    bernie.eigl@bccancer.bc.ca    Principal Investigator: Bernie Eigl, MD 收起 <<
NCT00000483 Cardiovascular Diseases ... 展开 >> Coronary Disease Heart Diseases Myocardial Infarction Myocardial Ischemia 收起 << Not Applicable Completed - -
NCT00000482 Cardiovascular Diseases ... 展开 >> Coronary Disease Heart Diseases Myocardial Infarction Myocardial Ischemia 收起 << Phase 3 Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.12mL

0.82mL

0.41mL

20.60mL

4.12mL

2.06mL

41.20mL

8.24mL

4.12mL
参考文献

[1]Xue J, Zhu W, et al. Activation of PPARα by clofibrate sensitizes pancreatic cancer cells to radiation through the Wnt/β-catenin pathway. Oncogene. 2017.

[2]WHO cooperative trial on primary prevention of ischaemic heart disease with clofibrate to lower serum cholesterol: final mortality follow-up. Report of the Committee of Principal Investigators. Lancet. 1984 Sep 15;2(8403):600-4.

[3]Willson TM, Brown PJ, Sternbach DD, Henke BR. The PPARs: from orphan receptors to drug discovery. J Med Chem. 2000 Feb 24;43(4):527-50

[4]Chen Y, Li W, Wang G, Burczynski FJ. Clofibrate Attenuates ROS Production by Lipid Overload in Cultured Rat Hepatoma Cells. J Pharm Pharm Sci. 2017;20(0):239-251

[5]Ibarra-Lara L, Sánchez-Aguilar M, Del Valle-Mondragón L, Soria-Castro E, Cervantes-Pérez LG, Pastelín-Hernández G, Sánchez-Mendoza A. Clofibrate improves myocardial ischemia-induced damage through regulation of renin-angiotensin system and favours a pro-vasodilator profile in left ventricle. J Pharmacol Sci. 2020 Dec;144(4):218-228

[6]Chen SH, Chao PM. Prenatal PPARα activation by clofibrate increases subcutaneous fat browning in male C57BL/6J mice fed a high-fat diet during adulthood. PLoS One. 2017 Nov 2;12(11):e0187507