Home Metabolism PPAR activator Gemfibrozil For research use only.

Gemfibrozil

Synonyms: CI-719

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

Gemfibrozil Chemical Structure

Gemfibrozil Chemical Structure

CAS No. 25812-30-0

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Gemfibrozil Related Products

Signaling Pathway

PPAR Signaling Pathways

PPAR Signaling Pathway

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
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06064539 Completed
Multiple Sclerosis
Sanofi
 May 18 2020 Phase 1
NCT03832595 Completed
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
Healthy Volunteers
Eli Lilly and Company
 December 2012 Phase 1
NCT01797198 Completed
Drug-Drug Interaction (DDI)|Healthy Subjects
Astellas Pharma Europe B.V.|Astellas Pharma Inc
 April 2012 Phase 1
NCT01913379 Completed
Healthy Subjects|Pharmacokinetics|Drug-Drug Interaction
Astellas Pharma Europe B.V.|Medivation Inc.|Astellas Pharma Inc
 August 2011 Phase 1

Chemical Information & Solubility

Molecular Weight 250.33 Formula

C15H22O3
CAS No. 25812-30-0 SDF Download Gemfibrozil SDF
Smiles CC1=CC(=C(C=C1)C)OCCCC(C)(C)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 50 mg/mL ( (199.73 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 50 mg/mL

Water : Insoluble


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In vivo
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