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Gemfibrozil

Catalog No. T1415 CAS 25812-30-0

Synonyms: CI-719, Jezil, Decrelip, Lopid

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).

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Gemfibrozil, CAS 25812-30-0

Pack Size	Availability	Price/USD
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

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Purity: 99.9%

Purity: 98.59%

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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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 47 mg/mL (187.8 mM)

Ethanol: 47 mg/mL (187.8 mM)

References and Literature

1. Prueksaritanont T, et al. J Pharmacol Exp Ther,2002, 301(3), 1042-1051. 2. Wang JS, et al. Drug Metab Dispos,2002, 30(12), 1352-1356. 3. Wen X, et al. Drug Metab Dispos,2001, 29(11), 1359-1361. 4. Pahan K, et al. J Biol Chem,2002, 277(48), 45984-45991.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library Anti-Neurodegenerative Disease Compound Library Drug Repurposing Compound Library Inhibitor Library Anti-Cancer Drug Library Pediatric Drug Library Nuclear Receptor Compound Library Drug-Fragment Library Anti-Obesity Compound Library

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Keywords

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

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