Gemfibrozil

Catalog No.S1729 Synonyms: CI-719

Gemfibrozil  Chemical Structure

Molecular Weight(MW): 250.33

Gemfibrozil is an activator of peroxisome proliferator-activated receptor-alpha (PPARα), used for the treatment of hypercholesterolemia and hypertriglyceridemia.

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In DMSO USD 130 In stock
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Biological Activity

Description Gemfibrozil is an activator of peroxisome proliferator-activated receptor-alpha (PPARα), used for the treatment of hypercholesterolemia and hypertriglyceridemia.
Targets
PPARα [1]
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 U373MG 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]

Protocol

Solubility (25°C)

In vitro DMSO 50 mg/mL (199.73 mM)
Ethanol 50 mg/mL (199.73 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 250.33
Formula

C15H22O3

CAS No. 25812-30-0
Storage powder
Synonyms CI-719

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02770222 Completed Healthy Subjects Actelion June 2016 Phase 1
NCT02638597 Recruiting Smoking Cessation University of Texas Southwestern Medical Center February 2015 Phase 2
NCT02230033 Completed Healthy Aragon Pharmaceuticals, Inc. September 2014 Phase 1
NCT02045056 Unknown status Preclinical Alzheimers Disease University of Kentucky May 2014 Early Phase 1
NCT01876810 Completed Nicotine Dependence Centre for Addiction and Mental Health February 2014 Phase 2
NCT01836198 Completed Healthy Volunteers Eli Lilly and Company May 2013 Phase 1

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PPAR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID