Name: Gemfibrozil
Brand: Selleck Chemicals
SKU: S1729
Rating: 5 (1 reviews)

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Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase Vitamin Carbohydrate Metabolism Mitochondrial Metabolism Drug Metabolite
Other PPAR Inhibitors	T0070907 GW9662 GW6471 WY-14643 (Pirinixic Acid) GSK3787 GW0742 AZ6102 Harmine Astaxanthin Eupatilin

Chemical Information, Storage & Stability

Molecular Weight	250.33	Formula	C₁₅H₂₂O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	25812-30-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	CI-719			Smiles	CC1=CC(=C(C=C1)C)OCCCC(C)(C)C(=O)O

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

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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

%DMSO+ %

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.

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	[1] https://pubmed.ncbi.nlm.nih.gov/12023536/ [2] https://pubmed.ncbi.nlm.nih.gov/12433802/ [3] https://pubmed.ncbi.nlm.nih.gov/11602509/ [4] https://pubmed.ncbi.nlm.nih.gov/12244038/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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Gemfibrozil PPAR activator

Chemical Structure

Molecular Weight: 250.33