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GW 4064

GW 4064 is a potent and selective agonist of the farnesoid X receptor (FXR), a nuclear receptor that plays a key role in bile acid, lipid, and glucose homeostasis.
This compound has been extensively studied for its therapeutic potential in the management of various metabolic and liver disorders, including non-alcoholic fatty liver disease (NAFLD) and primary biliary cirrhosis.
Reserchers have utilized GW 4064 to elucidate the underlying mechanisms and signaling pathways regulated by FXR activation, offering insights into the development of novel FXR-targeted therapies.
However, desiging robust and reproducible experimental protocols for GW 4064 research can be challanging.
PubCompare.ai's AI-driven platform can help locate the most reliable protocols from literature, preprints, and patents, leveraging advanced comparisons to identify the best protocols and products and enhance the accuracy and reproducibility of your GW 4064 studies.

Most cited protocols related to «GW 4064»

1
Genetic Mouse Models for Liver Research
Cited 6 times
E2F1+/+ and E2F1−/− mice were purchased from the Jackson Laboratory (Bar Harbor, ME, USA). C57BL/6 (WT), SHP−/− (SKO), SHP non-transgenic control (NC), hepatocyte specific SHP transgenic (STG), FXR−/− mice were described previously (14 (link), 21 (link), 22 (link)). The treatment of mice with DDC supplemented diet, bile duct ligation (BDL), and FXR synthetic ligand GW4064 has been described previously (19 (link), 20 (link), 22 (link)). Protocols for animal use were approved by the Institutional Animal Care and Use Committee at the University of Kansas Medical Center and University of Utah.
Zhang Y., Xu N., Xu J., Kong B., Copple B., Guo G.L, & Wang L. (2014). E2F1 is a novel fibrogenic gene that regulates cholestatic liver fibrosis through the Egr-1/SHP/EID1 network. Hepatology (Baltimore, Md.), 60(3), 919-930.
Publication 2014
Animals Animals, Transgenic Duct, Bile E2F1 protein, human GW 4064 Institutional Animal Care and Use Committees Ligands Ligation Mice, Laboratory Mice, Transgenic NOS2A protein, human Therapy, Diet
2
Fxr Activation and Bile Acid Metabolism
Cited 5 times
Mice were bred and maintained in the Laboratory Animal Research facility at the University of Kansas Medical Center in rooms under a 12-hr light/dark cycle. All protocols were approved by the IACUC. All experiments used 10–16 week old male mice and all mice were sacrificed within a 30-min period in the morning. In addition, all treatments were repeated twice.
Activation of Fxr in vivo was achieved by treatment with an Fxr synthetic agonist, GW4064, at 150 mg/kg. GW4064 or vehicle was administered by oral gavage at 6 PM, followed by a second administration at 8 AM next morning. Two hrs later, liver and ileum were harvested. The generation of purified Fgf15 has been reported previously.15 (link) Fgf15 protein was injected to mice through tail vein at a dosage of 10 μg/kg. Two hrs or indicated time points (for time course study) after the injection, livers were collected.
The total bile-acid pool size was determined by measuring bile acids of the small intestine, gallbladder, liver, and their contents. Ten-sixteen week-old mice were fed a chow diet with 2% cholestyramine for 10 days. Total bile acids were determined using a kit from Bio-quant Kits Inc. (San Diego, CA), and the pool size was expressed as micromoles of bile acids/100 g of body weight.
Kong B., Wang L., Chiang J.Y., Zhang Y., Klaassen C.D, & Guo G.L. (2012). Mechanism of Tissue-specific Farnesoid X Receptor in Suppressing the Expression of Genes in Bile-acid Synthesis in Mice. Hepatology (Baltimore, Md.), 56(3), 1034-1043.
Publication 2012
Animals Bile Acids Body Weight Diet Gallbladder GW 4064 Ileum Institutional Animal Care and Use Committees Intestines, Small Liver Males Mice, House Proteins Resin, Cholestyramine Tail Tube Feeding Veins
3
FXR and Resveratrol Modulate Liver Metabolism
Cited 4 times

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Publication 2009
Adenoviruses Adenovirus Vaccine Animals Corn oil FAT 16 GW 4064 Human Body Injections, Intraperitoneal Liver Males Mice, Congenic Mice, House Mice, Inbred BALB C Resveratrol Tail Veins
4
Fasting and FGF19 Metabolism Regulation
Cited 3 times
Male C57BL/6 mice and SHP-KO mice (8–12 weeks old) were fasted for 4–12 h and injected via the tail vein with vehicle or FGF19 (1 mg kg−1) at 9:00 a.m., and 2 h or 6 h later, livers were collected. For feeding experiments, mice were fasted for 12 h and then fed for 6 h and livers were collected for further analyses. For FXR activation studies, mice were fasted for 12 h and then treated intraperitoneally with GW4064 (30 mg kg−1 in corn oil) for 6 h. For dietary obese mouse studies, mice were fed normal chow or a HFD (Harlan Teklad, TD88137) with 25% of fructose (Sigma, F0127) in water for 11 weeks. Since 1C cycle metabolism is influenced by the circadian rhythm25 (link), mouse experiments were done at similar times of the day. AhR-KO and TetRE-CA-AHR transgenic mice12 (link) and SHP-KO21 (link) and FGF15-KO52 (link) mice have been described previously. For adenoviral experiments, mice were injected via the tail vein with 0.5–1.0 × 109 active viral particles in 100 µl phosphate-buffered saline (PBS) and 2–3 weeks later, the mice were killed and livers were collected. Injection of these viral doses does not elicit marked inflammatory responses20 (link). All experiments were approved by the Institutional Animal Care and Use and Biosafety Committees of the University of Illinois at Urbana-Champaign.
Kim Y.C., Seok S., Byun S., Kong B., Zhang Y., Guo G., Xie W., Ma J., Kemper B, & Kemper J.K. (2018). AhR and SHP regulate phosphatidylcholine and S-adenosylmethionine levels in the one-carbon cycle. Nature Communications, 9, 540.
Publication 2018
Adenoviruses Animals Animals, Transgenic Corn oil Diet Fructose GW 4064 Inflammation Liver Males Metabolism Mice, Inbred C57BL Mice, Laboratory Mice, Obese Phosphates Saline Solution Tail Veins Virion
5
Thermal Shift Assay for Ligand Binding
Cited 3 times
Thermal Shift assay was performed in clear 96-well plates (Invitrogen) using SYPRO Orange (Invitrogen Darmstadt, Germany) as dye. 10 μL of test compound (GW4064: final concentration 1 μM–500 μM, 100 μM for competitive testing; NSAIDs: 500 μM final concentration) in assay buffer (10 mM TRIS (pH 8.3), 5 mM DTT, 0.5 mM EDTA, 100 mM NaCl) were mixed with 10 μL of protein (final protein concentration 5 μM) in assay buffer and 5 μL of SYPRO Orange (5 × final concentration) in assay buffer. Temperature-dependent fluorescence increase reporting protein denaturation was measured in duplicates in an ICycler (Bio-Rad) from 20 to 90 °C in steps of 0.2 °C per minute at 300 nm excitation and 570 nm emission wavelength. Each experiment was independently repeated four times. The first derivative of the melting curves was calculated using the Graph Pad Prism 5 software.
Schmidt J., Klingler F.M., Proschak E., Steinhilber D., Schubert-Zsilavecz M, & Merk D. (2015). NSAIDs Ibuprofen, Indometacin, and Diclofenac do not interact with Farnesoid X Receptor. Scientific Reports, 5, 14782.
Publication 2015
Anti-Inflammatory Agents, Non-Steroidal Biological Assay Buffers Edetic Acid Fever Fluorescence GW 4064 prisma Protein Denaturation Proteins Sodium Chloride Tromethamine

Most recents protocols related to «GW 4064»

1
FXR-GW 4064 Complex Structural Insights
The crystal structures of the complex of farnesoid X receptor (FXR) and GW 4064 were downloaded from RCSB Protein Data Bank (PDB ID: 3dct, https://www.rcsb.org/) and prepared by SYBYL-X 2.0. The docking analysis was performed using the Surflex-Dock GeomX (SFXC) in SYBYL-X 2.0. The binding interaction was generated using PyMOL and ligplot.
Tang B., Tang L., Li S., Liu S., He J., Li P., Wang S., Yang M., Zhang L., Lei Y., Tu D., Tang X., Hu H., Ouyang Q., Chen X, & Yang S. (2023). Gut microbiota alters host bile acid metabolism to contribute to intrahepatic cholestasis of pregnancy. Nature Communications, 14, 1305.
Publication 2023
GW 4064 Rumex
2
FXR Transactivation Assay Protocol
Direct FXR activity was evaluated using the LanthaScreen™ TR-FRET Farnesoid X Receptor Coactivator Assay kit (Cat# PV4833, ThermoFisher Scientific). Briefly, prepare a 12-point 100× dilution series of GDCA (Cat#IG2290, Solarbio), CDCA (Cat#IC0300, Solarbio), GW4064 (Cat# HY-50108, MCE) and GUDCA (Cat#IG0840, Solarbio) in a 96-well plate by serial dilution, respectively. Dilute each 100× serial dilution to 2× using Complete Coregulator buffer G. Then, the 2× serial dilutions were mixed with FXR-LBD-glutathione S-transferase fusion protein, fluorecein-SRC2-2 coactivator peptide and Lantha-screen Tb anti-GST antibody (Cat# PV4833, ThermoFisher Scientific, 1:1500) in the 384-well assay plate. Mix the 384-well plate and the TR-FRET signal was evaluated in a Multi-Mode Microplate Reader (Varioskan Flash, Thermo Fisher). Calculate the TR-FRET ratio by dividing the emission signal at 520 nm by the emission signal at 495 nm. Generate a binding curve by plotting the emission ratio vs. [ligand].
Tang B., Tang L., Li S., Liu S., He J., Li P., Wang S., Yang M., Zhang L., Lei Y., Tu D., Tang X., Hu H., Ouyang Q., Chen X, & Yang S. (2023). Gut microbiota alters host bile acid metabolism to contribute to intrahepatic cholestasis of pregnancy. Nature Communications, 14, 1305.
Publication 2023
Antibodies, Anti-Idiotypic Biological Assay Buffers Chenodeoxycholic Acid Fluorescence Resonance Energy Transfer Glutathione S-Transferase GW 4064 Ligands Peptides Proteins Technique, Dilution
3
Modeling Intestinal Inflammation in Mice
All animal experiments were approved by the Institutional Animal Care and Use Committee of the University of Colorado Anschutz Medical Campus and all animals were treated humanely during the experimental techniques. All research was conducted in accordance with both the Declarations of Helsinki and Istanbul.
For the PNAC mouse model,4 (link),36 (link) C57BL/6 wild-type (WT) or Il1r−/− adult male mice (8 wk old, 22–25 g body weight) (Jackson Laboratories, Bar Harbor, ME) were treated sequentially with DSS in drinking water for 4 days, followed by PN for 14 days as reported36 (link) and described in Supplementary Experimental Procedures http://links.lww.com/HC9/A133. A subset of DSS-PN mice received the FXR agonist GW4064 (Tocris Bioscience, USA) i.v. 30 mg/kg, as reported.7 (link),36 (link) Another group of WT mice (8-wk old, 22–25 g body weight) (Jackson Laboratories, Bar Harbor, ME) were administrated i.p. injections of either 2.5 mg/kg/bw E. Coli lipopolysaccharides (LPS; from Escherichia coli 0111:B4; Sigma Aldrich, St. Louis, MO, USA) or 200ng recombinant mouse IL-1β (BD Biosciences, San Jose, CA) and 30 mg/kg/bw GW4064, as described in Supplementary Experimental Procedures http://links.lww.com/HC9/A133.7 (link),36 (link)
Ghosh S., Devereaux M.W., Anderson A.L., El Kasmi *.C, & Sokol R.J. (2023). Stat3 role in the protective effect of FXR Agonist in parenteral nutrition-associated cholestasis. Hepatology Communications, 7(3), e0056.
Publication 2023
Adult Animals Body Weight Escherichia coli GW 4064 Institutional Animal Care and Use Committees Interleukin-1 beta Males Mice, House
4
STAT3 Silencing and Lipid Modulators in Hepatocytes
HepG2 and Huh7 cells (ATCC, Manassas, VA) in culture were treated with 100 nM siRNA-STAT3 (cat: L-003544-00-0005, Dharmacon, Lafayette, CO) or a nontargeting siRNA (siRNA-NTC, cat: D-001810-10-05, Dharmacon) in the presence of Dharmafect transfection reagent for 24 hour. The next day, cells were treated with either combinations of 10 ng/mL IL-1β, 5 μM GW4064 or 10 μM stigmasterol acetate (Stig-Ac) and 10 μM sitosterol acetate (Sit-Ac) (Steraloids, Newport, RI) for 20 hours in DMEM-serum media with transfection mixture, as described.6 (link) In a separate set of experiment, in vitro IL-1β incubation was carried out in HepG2 and in Huh7 cells in culture by treating cells with 10 ng IL-1β (BD Biosciences, San Jose, CA) for 4 hours followed ±5 μM GW4064 overnight in DMEM media.
Ghosh S., Devereaux M.W., Anderson A.L., El Kasmi *.C, & Sokol R.J. (2023). Stat3 role in the protective effect of FXR Agonist in parenteral nutrition-associated cholestasis. Hepatology Communications, 7(3), e0056.
Publication 2023
Acetate Cell Culture Techniques Cells GW 4064 Interleukin-1 beta Interleukin-10 RNA, Small Interfering Serum sitosterol STAT3 Protein Stigmasterol Transfection
5
Inducing M2 Macrophages with Chitin
Female C57BL/6 mice were injected intraperitoneally with 50 µg of chitin particles from shrimp shells (C9752, Sigma-Aldrich) for 3 hr to induce M2 macrophages, followed by the first dosage of GW4064 (30 mg/kg) and 2 mg/kg LE540 or vehicle control. A second dose of GW4064 and LE540 at the same concentration as the first was then administered and the peritoneal macrophages collected for analysis.
Jaroonwitchawan T., Arimochi H., Sasaki Y., Ishifune C., Kondo H., Otsuka K., Tsukumo S.I, & Yasutomo K. (2023). Stimulation of the farnesoid X receptor promotes M2 macrophage polarization. Frontiers in Immunology, 14, 1065790.
Publication 2023
Chitin Females GW 4064 LE 540 Macrophage Macrophages, Peritoneal Mice, Inbred C57BL

Top products related to «GW 4064»

1
Gw4064 by Merck Group
Sourced in United States, Germany, Japan, United Kingdom
GW4064 is a laboratory reagent manufactured by Merck Group. It is a small molecule that functions as a selective agonist for the farnesoid X receptor (FXR). The core function of GW4064 is to activate FXR, a nuclear receptor that plays a role in the regulation of bile acid, lipid, and glucose metabolism.
2
Gw4064 by Bio-Techne
Sourced in United Kingdom, United States
GW4064 is a synthetic agonist of the nuclear receptor farnesoid X receptor (FXR). It serves as a molecular tool for studying the biological functions and signaling pathways associated with FXR activation.
3
Fetal bovine serum (fbs) by Thermo Fisher Scientific
Sourced in United States, China, United Kingdom, Germany, Australia, Japan, Canada, Italy, France, Switzerland, New Zealand, Brazil, Belgium, India, Spain, Israel, Austria, Poland, Ireland, Sweden, Macao, Netherlands, Denmark, Cameroon, Singapore, Portugal, Argentina, Holy See (Vatican City State), Morocco, Uruguay, Mexico, Thailand, Sao Tome and Principe, Hungary, Panama, Hong Kong, Norway, United Arab Emirates, Czechia, Russian Federation, Chile, Moldova, Republic of, Gabon, Palestine, State of, Saudi Arabia, Senegal
Fetal Bovine Serum (FBS) is a cell culture supplement derived from the blood of bovine fetuses. FBS provides a source of proteins, growth factors, and other components that support the growth and maintenance of various cell types in in vitro cell culture applications.
4
Gw4064 by Selleck Chemicals
Sourced in United States
GW4064 is a laboratory chemical compound. It functions as a farnesoid X receptor (FXR) agonist.
5
Lipofectamine 2000 by Thermo Fisher Scientific
Sourced in United States, China, Germany, United Kingdom, Canada, Japan, France, Italy, Switzerland, Australia, Spain, Belgium, Denmark, Singapore, India, Netherlands, Sweden, New Zealand, Portugal, Poland, Israel, Lithuania, Hong Kong, Argentina, Ireland, Austria, Czechia, Cameroon, Taiwan, Province of China, Morocco
Lipofectamine 2000 is a cationic lipid-based transfection reagent designed for efficient and reliable delivery of nucleic acids, such as plasmid DNA and small interfering RNA (siRNA), into a wide range of eukaryotic cell types. It facilitates the formation of complexes between the nucleic acid and the lipid components, which can then be introduced into cells to enable gene expression or gene silencing studies.
6
Dulbecco modified eagle medium (dmem) by Thermo Fisher Scientific
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DMEM (Dulbecco's Modified Eagle's Medium) is a cell culture medium formulated to support the growth and maintenance of a variety of cell types, including mammalian cells. It provides essential nutrients, amino acids, vitamins, and other components necessary for cell proliferation and survival in an in vitro environment.
7
Gw4064 by Cayman Chemical
Sourced in United States
GW4064 is a synthetic compound that acts as a selective agonist for the farnesoid X receptor (FXR). FXR is a nuclear receptor that plays a key role in regulating bile acid, lipid, and glucose metabolism. GW4064 can be used in research applications to study the physiological functions of FXR and its potential therapeutic implications.
8
Hepg2 cell by American Type Culture Collection
Sourced in United States, China, United Kingdom, Germany, Japan, Canada
HepG2 cells are a well-established human hepatocellular carcinoma cell line derived from the liver tissue of a 15-year-old Caucasian male. They are commonly used in cell-based assays and research studies related to liver function, metabolism, and toxicology.
9
Trizol reagent by Thermo Fisher Scientific
Sourced in United States, China, Japan, Germany, United Kingdom, Canada, France, Italy, Australia, Spain, Switzerland, Netherlands, Belgium, Lithuania, Denmark, Singapore, New Zealand, India, Brazil, Argentina, Sweden, Norway, Austria, Poland, Finland, Israel, Hong Kong, Cameroon, Sao Tome and Principe, Macao, Taiwan, Province of China, Thailand
TRIzol reagent is a monophasic solution of phenol, guanidine isothiocyanate, and other proprietary components designed for the isolation of total RNA, DNA, and proteins from a variety of biological samples. The reagent maintains the integrity of the RNA while disrupting cells and dissolving cell components.
10
Dual luciferase reporter assay system by Promega
Sourced in United States, China, Germany, United Kingdom, Switzerland, Japan, France, Italy, Spain, Austria, Australia, Hong Kong, Finland
The Dual-Luciferase Reporter Assay System is a laboratory tool designed to measure and compare the activity of two different luciferase reporter genes simultaneously. The system provides a quantitative method for analyzing gene expression and regulation in transfected or transduced cells.

More about "GW 4064"

Farnesoid X Receptor (FXR) Agonist GW 4064: Uncovering Metabolic Insights and Optimizing Research Protocols GW 4064 is a potent and selective agonist of the farnesoid X receptor (FXR), a key nuclear receptor that plays a critical role in regulating bile acid, lipid, and glucose homeostasis.
This compound has been extensively studied for its therapeutic potential in the management of various metabolic and liver disorders, including non-alcoholic fatty liver disease (NAFLD) and primary biliary cirrhosis.
Researchers have utilized GW 4064 to elucidate the underlying mechanisms and signaling pathways regulated by FXR activation, offering valuable insights into the development of novel FXR-targeted therapies.
However, designing robust and reproducible experimental protocols for GW 4064 research can be challenging.
PubCompare.ai's AI-driven platform can help researchers optimize their GW 4064 studies by providing access to the most reliable protocols from literature, preprints, and patents.
By leveraging advanced comparisons, the platform can identify the best protocols and products, enhancing the accuracy and reproducibility of your research.
When conducting GW 4064 experiments, it's important to consider the use of complementary reagents and cell lines, such as FBS, Lipofectamine 2000, DMEM, HepG2 cells, TRIzol reagent, and the Dual-Luciferase Reporter Assay System.
These tools can help you gain a comprehensive understanding of the molecular mechanisms and signaling pathways regulated by FXR activation.
Start enhancing your GW 4064 research today with the help of PubCompare.ai's AI-driven platform.
Discover the most reliable protocols, optimize your experimental design, and unlock new insights into the therapeutic potential of this FXR agonist.