生物活性 | |||
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描述 | PPAR (peroxisome proliferator-activated receptors) are ligand-activated transcription factors of nuclear hormone receptor superfamily comprising of PPARα, PPARγ, and PPARβ/δ[3]. Gemfibrozil is a PPARα and PPARγ agonist (EC50s = 193.3 and 147.8 µM, respectively)[4]. In vivo, gemfibrozil (50 mg/kg, p.o.) reduces serum total cholesterol, triglyceride, and LDL levels in a rat model of high-cholesterol diet-induced hyperlipidemia[5]. Gemfibrozil (100 mg/kg per day) reduces atherosclerotic plaque area, superoxide production, and expression of the genes encoding the NF-κB subunit p65 and chemokine (C-C) motif ligand 2 (CCL2) in ApoE-/- mice. Formulations containing gemfibrozil have been used in the treatment of high cholesterol[6]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.99mL 0.80mL 0.40mL |
19.97mL 3.99mL 2.00mL |
39.95mL 7.99mL 3.99mL |
参考文献 |
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