Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Gemfibrozil (CI-719) interacts with peroxisome proliferator-activated receptors (PPARalpha) resulting in PPARalpha-mediated stimulation of fatty acid oxidation and an increase in lipoprotein lipase (LPL) synthesis. Gemfibrozil is a fibric acid derivative with hypolipidemic effects. This enhances triglyceride-rich lipoprotein clearance and reduces the expression of apolipoprotein C-III (apoC-III). The reduction in hepatic production of apoC-III result in the subsequent reduction of serum levels of very-low-density-lipoprotein cholesterol (VLDL-C). In addition, gemfibrozil-mediated PPARalpha stimulation of apoA-I and apoA-II expression results in an increase in high-density lipoprotein cholesterol (HDL-C).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | In stock | $ 30.00 | |
50 mg | In stock | $ 38.00 | |
100 mg | In stock | $ 50.00 | |
200 mg | In stock | $ 63.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 50.00 |
Description | Gemfibrozil (CI-719) interacts with peroxisome proliferator-activated receptors (PPARalpha) resulting in PPARalpha-mediated stimulation of fatty acid oxidation and an increase in lipoprotein lipase (LPL) synthesis. Gemfibrozil is a fibric acid derivative with hypolipidemic effects. This enhances triglyceride-rich lipoprotein clearance and reduces the expression of apolipoprotein C-III (apoC-III). The reduction in hepatic production of apoC-III result in the subsequent reduction of serum levels of very-low-density-lipoprotein cholesterol (VLDL-C). In addition, gemfibrozil-mediated PPARalpha stimulation of apoA-I and apoA-II expression results in an increase in high-density lipoprotein cholesterol (HDL-C). |
Targets&IC50 | CYP2C9:5.8 μM(Ki), 2C19:24 μM(Ki), 1A2:82 μM(Ki), 2C8:69 μM(Ki) |
In vitro | Gemfibrozil exerts a minimal inhibitory effect on CYP3A-mediated simvastatin hydroxy acid (SVA) oxidation, but does inhibit SVA glucuronidation in dog and human liver microsomes. [1] Gemfibrozil markedly inhibits M-23 formation, with a K(i) (IC(50)) value of 69 (95) mM, whereas inhibition of M-1 formation is weaker with a K(i) (IC(50)) value of 273 mM in human liver microsomes. [2] Gemfibrozil strongly and competitively inhibits CYP2C9 activity, with a K(i) (IC(50)) value of 5.8 (9.6) mM. Gemfibrozil exhibits somewhat smaller inhibitory effects on CYP2C19 and CYP1A2 activities, with K(i) (IC(50)) values of 24 (47) mM and 82 (136) mM, respectively. [3] Gemfibrozil, a lipid-lowering drug, inhibits cytokine-induced production of NO and the expression of inducible nitric-oxide synthase (iNOS) in human U373 mg astroglial cells and primary astrocytes. Gemfibrozil induces peroxisome proliferator-responsive element (PPRE)-dependent luciferase activity, which is inhibited by the expression of DeltahPPAR-alpha, the dominant-negative mutant of human PPAR-alpha. Gemfibrozil strongly inhibits the activation of NF-kappaB, AP-1, and C/EBPbeta but not that of gamma-activation site (GAS) in cytokine-stimulated astroglial cells. [4] |
In vivo | Gemfibrozil treatment significantly reduces (2-3-fold) the plasma clearance of SVA and the biliary excretion of SVA glucuronide (together with its cyclization product SV), but not the excretion of a major oxidative metabolite of SVA in dogs. [1] |
Synonyms | CI-719, Jezil, Decrelip, Lopid |
Molecular Weight | 250.33 |
Formula | C15H22O3 |
CAS No. | 25812-30-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 47 mg/mL (187.8 mM)
Ethanol: 47 mg/mL (187.8 mM)
You can also refer to dose conversion for different animals. More
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Gemfibrozil 25812-30-0 DNA Damage/DNA Repair GPCR/G Protein Metabolism Neuroscience P450 PPAR Adrenergic Receptor Peroxisome proliferator-activated receptors Inhibitor inhibit CI719 CI 719 Cytochrome P450 CYPs CI-719 Jezil Decrelip Lopid inhibitor