Catalog No.S1729 Synonyms: CI-719

For research use only.

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

Gemfibrozil  Chemical Structure

CAS No. 25812-30-0

Purity & Quality Control

Choose Selective PPAR Inhibitors

Other PPAR Products

Biological Activity

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

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 250.33


CAS No. 25812-30-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC(=C(C=C1)C)OCCCC(C)(C)C(=O)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

(data from, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Gemfibrozil | Gemfibrozil ic50 | Gemfibrozil price | Gemfibrozil cost | Gemfibrozil solubility dmso | Gemfibrozil purchase | Gemfibrozil manufacturer | Gemfibrozil research buy | Gemfibrozil order | Gemfibrozil mouse | Gemfibrozil chemical structure | Gemfibrozil mw | Gemfibrozil molecular weight | Gemfibrozil datasheet | Gemfibrozil supplier | Gemfibrozil in vitro | Gemfibrozil cell line | Gemfibrozil concentration | Gemfibrozil nmr