Gemfibrozil is an agonist of PPARα. It can act as a hyperlipidemic agent that elevates plasma HDL and lowers triglycerides.
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产品名称 | PPARα ↓ ↑ | PPARβ/δ ↓ ↑ | PPARγ ↓ ↑ | PPARδ ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Fenofibric acid | ✔ | 98% | |||||||||||||||||
GW6471 |
++
PPARα, IC50: 0.24 μM |
99%+ | |||||||||||||||||
GSK3787 |
++
PPARδ, pIC50: 6.6 |
++
PPARδ, pIC50: 6.6 |
99%+ | ||||||||||||||||
FH535 | ✔ | 98%+ | |||||||||||||||||
GW9662 |
+++
PPARα, IC50: 32 nM |
+++
PPARγ, IC50: 3.3 nM |
98% | ||||||||||||||||
T0070907 |
++++
PPARγ, IC50: 1 nM |
98% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
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]. |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 25812-30-0 |
分子式 | C15H22O3 |
分子量 | 250.33 |
别名 | CI-719 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,Room Temperature |
溶解度 |
DMSO: 105 mg/mL(419.45 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 |
动物实验配方 |