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Gemfibrozil PPAR activator

Cat.No.S1729

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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Quality Control

Batch: Purity: 99.99%
99.99

Solubility

In vitro
Batch:

DMSO : 50 mg/mL (199.73 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 50 mg/mL

Water : Insoluble

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 250.33 Formula

C15H22O3

Storage (From the date of receipt)
CAS No. 25812-30-0 Download SDF Storage of Stock Solutions

Synonyms CI-719 SMILES CC1=CC(=C(C=C1)C)OCCCC(C)(C)C(=O)O

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Mechanism of Action

Targets/IC50/Ki
PPARα
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. This compound 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. It strongly and competitively inhibits CYP2C9 activity, with a K(i) (IC(50)) value of 5.8 (9.6) mM. This chemical 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. This compound, 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. It 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. This chemical 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.
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.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/12244038/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-08-19)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05931484 WITHDRAWN
Parkinson Disease
Forest Hills Lab
2027-11-01 PHASE2
NCT06809608 COMPLETED
Healthy Participants
Hoffmann-La Roche
2025-02-13 PHASE1
NCT06392659 COMPLETED
Pain
Vertex Pharmaceuticals Incorporated
2024-05-02 PHASE1
NCT05932303 COMPLETED
Healthy Participants
Bristol-Myers Squibb
2023-07-12 PHASE1
NCT05959447 COMPLETED
Cough; Healthy
Bellus Health Inc. - a GSK company
2023-07-26 PHASE1
NCT04956627 COMPLETED
Healthy Participants
Bristol-Myers Squibb
2021-07-28 PHASE1

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