Gemfibrozil

For research use only.

Catalog No.S1729 Synonyms: CI-719

Gemfibrozil  Chemical Structure

CAS No. 25812-30-0

Gemfibrozil (CI-719) is an activator of peroxisome proliferator-activated receptor-alpha (PPARα), used for the treatment of hypercholesterolemia and hypertriglyceridemia.

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Biological Activity

Description Gemfibrozil (CI-719) 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

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Chemical Information

Molecular Weight 250.33
Formula

C15H22O3

CAS No. 25812-30-0
Storage powder
in solvent
Synonyms CI-719
Smiles CC1=CC(=C(C=C1)C)OCCCC(C)(C)C(=O)O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03832595 Enrolling by invitation Other: Intervention Arm|Other: Usual Care Chronic Kidney Diseases University of Pittsburgh|Vanderbilt University Medical Center|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) May 1 2019 Not Applicable
NCT01736254 Completed Drug: Evacetrapib|Drug: Gemfibrozil Healthy Volunteers Eli Lilly and Company December 2012 Phase 1
NCT01797198 Completed Drug: ASP3652|Drug: Gemfibrozil|Drug: Repaglinide Drug-Drug Interaction (DDI)|Healthy Subjects Astellas Pharma Europe B.V.|Astellas Pharma Inc April 2012 Phase 1
NCT01913379 Completed Drug: MDV3100|Drug: Gemfibrozil|Drug: Itraconazole Healthy Subjects|Pharmacokinetics|Drug-Drug Interaction Astellas Pharma Europe B.V.|Medivation Inc.|Astellas Pharma Inc August 2011 Phase 1
NCT01083212 Completed Drug: AZD1656|Drug: Gemfibrozil|Drug: Placebo Type 2 Diabetes Mellitus AstraZeneca March 2010 Phase 1
NCT00566865 Completed Drug: placebo for gemfibrozil|Drug: gemfibrozil Type 2 Diabetes Mellitus Elixir Pharmaceuticals November 2007 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