Gemfibrozil

Manufactured by Merck Group

Sourced in United States

Gemfibrozil is a pharmaceutical product developed and manufactured by Merck Group. It is a type of drug classified as a fibric acid derivative. Gemfibrozil is used to help manage certain types of high cholesterol and triglyceride levels in the blood.

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Lab products found in correlation

28 protocols using gemfibrozil

Investigating PPAR Receptors and Neuronal Markers

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Rabbit polyclonal anti-PPARα antibody (Abcam; Cat# ab189159; WB and IHC), mouse anti-NeuN antibody (Millipore; Cat# MAB377), rabbit polyclonal anti-PPARβ antibody (Abcam; Cat # ab8937; WB and IHC), anti-PPARγ antibody (Abcam; Cat# ab66343; WB and IHC), anti-NMDAR2A antibody (Cell Signaling for WB at a dilution of 1:1000, Cat #4205; Abcam for IHC, Cat# ab169873), anti-GluR1 antibody (Cell Signaling for WB at a dilution of 1:1000, Cat #13185; Abcam for IHC, Cat # ab131507), anti-CREB antibody ( Cell Signaling for WB at a dilution of 1:1000 and IC at a dilution of 1:200, Cat# 9104), and anti-Arc antibody (Abcam for WB at a dilution of 1:1000, Cat # ab118929) were used in this study. Different pharmacological compounds including 9-octadecenamide (Cat#O2136), hexadecanamide (Cat#S350435), 2,4-bis(α,α-dimethyl benzyl) phenol (Cat #372129), gemfibrozil (Cat #G9518), clofibrate (Cat# C6643), fenofibrate (Cat# F6020), GW9662 (Cat# M6191), WY-14643 (Cat# C7081), and MTT-based toxicity assay kit (Stock No. TOX-1) were purchased from Sigma-Aldrich. GST-PPARα-LBD and GST-PPARβ-LBD were purchased from Protein One. On the other hand, 3-hydroxy 2, 2-dimethyl butyric acid ethyl ester (Cat# sc-216452) was purchased from Santa Cruz.

Roy A., Kundu M., Jana M., Mishra R.K., Yung Y., Luan C.H., Gonzalez F.J, & Pahan K. (2016). Identification and characterization of PPARα ligands in the hippocampus. Nature chemical biology, 12(12), 1075-1083.

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Virus Propagation and Cell Maintenance

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MDCK, HEp-2, LLC-MK₂ and A549 cells were maintained in Dulbecco’s modified Eagle’s medium (DMEM; Corning) supplemented with 8% fetal calf serum (FCS; Life Technologies), 2% HEPES (Gibco) and 0.1% Gentamicin (Life Technologies). Recombinant A/California/04/2009 (H1N1) virus was rescued previously by a 12-plasmid rescue system (Hayashi et al., 2016 (link)) and propagated in eggs. A/Victoria/361/2011 (H3N2) virus was kindly provided by Dr. David Topham (University of Rochester) and propagated in MDCK cells in DMEM supplemented with 0.15% bovine serum albumin (BSA) and acetylated trypsin at 2 μg/ml. RSV (strain A2) were grown in HEp-2 cells in DMEM supplemented with 2% FCS. hPIV1 (strain C-35) were grown in LLC-MK₂ cells in DMEM supplemented with 0.15% BSA and acetylated trypsin at 2 μg/ml. Gemfibrozil (Sigma) and Lovastatin (Sigma) were dissolved in dimethyl sulfoxide (DMSO, Sigma) to make 200 mM and 20 mM stock solutions. Water-soluble cholesterol in powder form suitable for cell culture was purchased from Sigma.

Bajimaya S., Frankl T., Hayashi T, & Takimoto T. (2017). Cholesterol is required for stability and infectivity of influenza A and respiratory syncytial viruses. Virology, 510, 234-241.

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Bile Acid Profiling in Liver Disease

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Gemfibrozil, taurocholic acid (TCA), tauro-α-muricholic acid (TαMCA), tauro-β-muricholic acid (TβMCA), and chlorpropamide were purchased from Sigma (St. Louis, MO). TCA-d5 sodium was provided by Unites States Biological Corp. (Salem, MA). Alanine aminotransferase (ALT, LOT: LB261301301, C164–0A), aspartate aminotransferase (AST, LOT: LI291101, C154–0B), and alkaline phosphatase (ALP, LOT: LF050801E, C174–0C) assay kits were purchased from Catachem (Bridgeport, CT). Colorimetric triglyceride (TG, LOT: DE976, 461–08992) and total bile acid (TBA, LOT: KM996, 990–23491) kits were from Wako Chemicals (Richmond, VA). Standard authentic compounds 1-palmitoyl-sn-glycero-3-phosphocholine (LPC 16:0), 1-stearoyl-sn-glycero-3-phosphocholine (LPC18:0), 1-ole- oyl-2-hydroxy-sn-glycero-3-phosphocholine (LPC18:1, 9Z) were obtained from Avanti Polar Lipids, Inc. (Alabaster, AL). Organic reagents acetonitrile and formic acid were of the highest obtainable grade commercially available.

Liu A., Krausz K.W., Fang Z.Z., Brocker C., Qu A, & Gonzalez F.J. (2014). Gemfibrozil disrupts lysophosphatidylcholine and bile acid homeostasis via PPARα and its relevance to hepatotoxicity. Archives of toxicology, 88(4), 983-996.

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Preparation of Chemical Stock Solutions

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Prochloraz (purity 99.1%, CAS 67747-09-5), tributyltin (TBT) chloride (96%, CAS 1461-22-9), tetrabromobisphenol A (TBBPA, 2,2-bis(3,5-dibromo-4-hydroxyphenyl)propane) (97%, CAS 79-94-7), perfluorooctanoic acid (PFOA) (96%, CAS 335-67-1), imazalil (99.7%, CAS 35554-44-0), butralin (99.8%, CAS 33629-47-9), clofibrate (CAS 637-07-0), and gemfibrozil (CAS 25812-30-0) were obtained from Sigma-Aldrich (St. Louis, MO). Tetrachlorobisphenol A (TCBPA, 2,2-bis(3,5-dichloro-4-hydroxyphenyl)propane) (95%, CAS 79-95-8) was purchased from TCI America (Portland, OR). All chemicals were dissolved and diluted in DMSO to make 1000× stock solutions.

Kalasekar S.M., Zacharia E., Kessler N., Ducharme N.A., Gustafsson J.Å., Kakadiaris I.A, & Bondesson M. (2014). Identification of environmental chemicals that induce yolk malabsorption in zebrafish using automated image segmentation. Reproductive toxicology (Elmsford, N.Y.), 55, 20-29.

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Buspirone Metabolism Assay Protocol

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Buspirone hydrochloride (BP·HCl), Tes (purity > 98%), 6β-hydroxytestosterone (purity > 98%), and gemfibrozil (used as an internal standard, purity > 98%) were purchased from Sigma-Aldrich (St. Louis, MO, USA). 1-PP, 6′-OH-BP, and SKF-525A hydrochloride (used as a positive control drug) were obtained from Toronto Research Chemicals, Inc. (Toronto, CA). An NADPH regenerating system was purchased from BD Gentest Corp. (Woburn, MA, USA). HPLC-grade acetonitrile for liquid chromatography was purchased from Merck (Darmstadt, Germany). Deionized water was prepared by a Millipore Milli-Q Plus system (Millipore Bedford, MA, USA). All other chemicals used were of analytical reagent grade or better.

Wu J., Cheng Z., Zhu L., Lu L., Zhang G., Wang Y., Xu Y., Lin N, & Liu Z. (2014). Coadministration of Pinellia ternata Can Significantly Reduce Aconitum carmichaelii to Inhibit CYP3A Activity in Rats. Evidence-based Complementary and Alternative Medicine : eCAM, 2014, 734867.

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Characterization of Drug-Transporter Interactions

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Enalapril maleate was purchased from Tokyo Chemical Industry Co., Ltd. (Shanghai, China). Enalaprilat, gemfibrozil, telmisartan, repaglinide, glimepiride, febuxostat, valsartan, and diclofenac sodium were purchased from Sigma-Aldrich (St. Louis, MO, USA). Dulbecco’s modified Eagle’s medium (DMEM) and fetal bovine serum (FBS) were purchased from Hyclone (Logan, UT, USA) and trypsin was from Genom (Hangzhou, China). Twenty four-well plates biocoated with poly-D-lysine was obtained from BD Biosciences (San Jose, CA, USA). Hanks’ balance salt solution (HBSS) containing 1.3 mM CaCl₂, 0.5 mM MgCl₂, 0.4 mM MgSO₄, 5.4 mM KCl, 0.4 mM KH₂PO₄, 137 mM NaCl, 4.2 mM NaHCO₃, 0.3 mM Na₂HPO₄, 10 mM HEPES, and 5 mM D-glucose was prepared in house. All other reagents and chemicals were of analytical grade or of the highest quality available commercially.

Ni Y., Duan Z., Zhou D., Liu S., Wan H., Gui C, & Zhang H. (2020). Identification of Structural Features for the Inhibition of OAT3-Mediated Uptake of Enalaprilat by Selected Drugs and Flavonoids. Frontiers in Pharmacology, 11, 802.

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NMR Spectroscopy of Lipid-Lowering Drugs

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The spectra were recorded at 300 K on a Bruker Avance III 400 MHz NMR with a broadband probe and analyzed using the Bruker Topspin software package [24 ]. Bezafibrate (Sigma lot: 046k1113), gemfibrozil (Sigma lot: 65H0084), and clofibric acid (Aldrich lot: 01220BT) were purchased commercially and used without further modification. Fen was synthesized from fenofibrate as previously reported and characterized [12 (link)]. Each compound was dissolved in acetone-d₆ (99.9 atom % D) with 0.3% TMS, purchased from Sigma. ¹H spectra utilized the zg30 pulse program [24 ], with digital quad detection (DQD) acquisition mode. For each spectrum, 128 scans were collected with a D1 delay of 2.0 s; a 90° pulse time of 7.83 μs; a sweep width (sw) range of 20.55-20.68 ppm; o1 signal range of 2470.79-2471.09 Hz; and the receiver gain set to 143.7 for Beza, 645.1 for Clo, 12.7 for Gem, and 181 for Fen. ¹³C spectra were run proton decoupled (pulse program zgpg30) with qsim acquisition mode, 1024 scans, a 90° pulse time of 14.90 μs, and a D1 delay of 2.0 s. The sw range was 238.32-238.88 ppm, the ¹³C o1 range was 10060.80-10061.31 Hz, the ¹H o2 range was 1600.52-1600.60 Hz, and the receiver gain was 181 for Beza, 203.2 for Clo, and 2050 for Fen and Gem.

Miller C., Schildcrout S., Mettee H, & Balendiran G. (2022). Molecular dynamics of fibric acids. European journal of chemistry (Print), 13(2), 186-195.

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Gemfibrozil Inclusion Complex Formation

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Gemfibrozil was purchased from Sigma (Madrid, Spain). β-CD was from Roquette S.A. (Lestrem, France), Meβ- (DS ≈ 12) and HPβ-CD (DS ≈ 4,5) from Cyclolab (Budapest, Hungary). All other reagents and solvents were from Panreac (Barcelona, Spain).

Zornoza A., Vélaz I., González-Gaitano G, & Martínez-Ohárriz M.C. (2022). A Comprehensive Study of Gemfibrozil Complexation with β-Cyclodextrins in Aqueous Solution Using Different Analytical Techniques. International Journal of Molecular Sciences, 23(24), 16119.

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Modeling ARPE-19 Cell Barrier Responses

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ARPE-19 cells (American Type Culture Collection, Manassas, VA) at passages 3–15 were maintained in DMEM supplemented with 10% fetal bovine serum (Sigma-Aldrich, St. Louis, MO) at 37°C under 5% CO₂ and 95% air. A confluent monolayer barrier was established following the previously published methods.^{18 (link),19 (link)} Cells were seeded onto 24-well semipermeable transwell plates and cultured in growth medium for 18–21 days, when a tight barrier was formed; the medium was refreshed every 2–3 days. The cells were then switched to serum-free medium (SFM) overnight before treatments with lipoproteins and/or other agents. Conventional cell culture was also used to complement the barrier model for mechanistic studies. Fenofibrate, fenofibric acid, gemfibrozil, bezafibrate, WY14643, GW6471, and Compound C (all from Sigma-Aldrich, St. Louis, MO) were spiked into culture media or into transwell inserts (i.e., apical side of the RPE barrier). Four-hydroxynonenal (4-HNE; Cayman Chemical, Ann Arbor, MI) was assessed as a potentially convenient means to simulate the effects of HOG-LDL. The blocking antibody for lectin-type oxidized LDL receptor 1 (LOX-1) was obtained from Thermo-Fisher Scientific (Raleigh, NC).

Fu D., Yu J.Y., Connell A.R., Hookham M.B., McLeese R.H, & Lyons T.J. (2020). Effects of Modified Low-Density Lipoproteins and Fenofibrate on an Outer Blood-Retina Barrier Model: Implications for Diabetic Retinopathy. Journal of Ocular Pharmacology and Therapeutics, 36(10), 754-764.

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Synthesis of Metal Nanoparticles

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Iron (III) chloride, tungsten hexachloride (WCl₆), polyethylene glycol (PEG), hydrochloric acid, copper (II) acetate (Cu(CH₃COO)₂), potassium ferricyanide (K₃Fe(CN)₆), polyvinyl pyrrolidone (PVP), and ethanol were purchased from Merck (Darmstadt, Germany). Silver nitrate, Tamoxifen, and Gemfibrozil were obtained from Sigma Aldrich (St. Louis, MO, USA). All the materials were used without further purification. Deionized water was used to prepare the aqueous solutions in this study.

Sayadi M.H., Ahmadpour N, & Homaeigohar S. (2021). Photocatalytic and Antibacterial Properties of Ag-CuFe2O4@WO3 Magnetic Nanocomposite. Nanomaterials, 11(2), 298.

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