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    Gemfibrozil
    Gemfibrozil

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0835
    CAS #: 25812-30-0Purity ≥98%

    Description: Gemfibrozil (Pilder; CI-719; CI719; CI 719; Lopid; Jezil; Lipur; Trialmin) is a potent anti-hypertriglyceridemic/lipid lowering drug acting as an activator/agonist of peroxisome proliferator-activated receptor-alpha (PPARα). It has been approved for the treatment of hypercholesterolemia and hypertriglyceridemia.  

    References: J Pharmacol Exp Ther. 2002 Jun;301(3):1042-51; Drug Metab Dispos. 2001 Nov;29(11):1359-61.

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    Molecular Weight (MW)250.33
    FormulaC15H22O3
    CAS No.25812-30-0
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 50 mg/mL (199.7 mM)
    Water: <1 mg/mL
    Ethanol: 50 mg/mL (199.7 mM)
    Solubility (In vivo)

    Chemical Name: 5-(2,5-dimethylphenoxy)-2,2-dimethylpentanoic acid

    InChi Key: HEMJJKBWTPKOJG-UHFFFAOYSA-N

    InChi Code: InChI=1S/C15H22O3/c1-11-6-7-12(2)13(10-11)18-9-5-8-15(3,4)14(16)17/h6-7,10H,5,8-9H2,1-4H3,(H,16,17)

    SMILES Code: CC1=CC(=C(C=C1)C)OCCCC(C)(C)C(=O)O

    SynonymsPilder; PMS Gemfibrozil; CI-719; CI719; CI 719; PMS-Gemfibrozil; Gemfibrozil; Lopid; 5-(2,5-Dimethylphenoxy)-2,2-dimethylpentanoic acid; Jezil; Lipur; Trialmin; SBPA Gemfibrozil


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    In Vitro

    In vitro activity: 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. 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. 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. 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


    Kinase Assay: Activities of CYP3A4 (testosterone 6β-hydroxylation) and CYP2C8 (paclitaxel 6α-hydroxylation) are determined. The marker substrate concentrations used, 25 μM testosterone and 1 to 5 μM paclitaxel, are comparable with or around the Km values of the reactions. Gemfibrozil is either coincubated at 37°C for 15 min with the marker substrate and NADPH (1 mM) before the reaction is initiated with human liver microsomes (0.1 mg/mL) or preincubated with human liver microsomes and NADPH for 15 min before adding the marker substrate.


    Cell Assay: Briefly, 400 μL of culture supernatant is allowed to react with 200 μL of Griess reagent and incubated at room temperature for 15 min. The optical density of the assay samples is measured spectrophotometrically at 570 nm. Fresh culture medium serves as the blank in all experiments. Nitrite concentrations are calculated from a standard curve derived from the reaction of NaNO2 in the assay.

    In VivoGemfibrozil 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. 
    Animal modelMice
    Formulation & DosageMice are given vehicle or gemfibrozil beginning 3 days before SCI to ensure drug availability at the time of the injury (n=5-6/group). The drug is delivered orally by dissolving it in ethanol (0.25% w/w of gemfibrozil) and coating food pellets such that each animal receives appr 62 mg/kg/day; chow for control groups is treated with ethanol. Ethanol for each group is allowed to completely evaporate before giving the food to the animals. In addition, animals receive an intraperitoneal injection of vehicle or gemfibrozil (500 µg dissolved in 200 µL PBS) 1 h after the injury, and then continued to receive the drug in their food until the end of the study (28 days post-injury)
    References

     J Pharmacol Exp Ther. 2002 Jun;301(3):1042-51; Drug Metab Dispos. 2001 Nov;29(11):1359-61.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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