GW4064
Catalog No.S2782
Molecular Weight(MW): 542.84
GW4064 is an agonist of farnesoid X receptor (FXR) with EC50 of 65 nM in CV1 cell line and displays no activity at other nuclear receptors at concentrations up to 1 μM.
4 Customer Reviews
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FXR agonist GW4064 reduced the association between β-Catenin/TCF4 complex and the TCF binding sites from Cyclin D1 promoter. ChIP analysis was carried out using antibodies against TCF4, β-Catenin, or normal IgG in lysates from Huh7 cells.
Oncotarget, 2015, 6: 4226-38 . GW4064 purchased from Selleck.
Myocardial infarct size and myocardial fibrosis were determined by Masson’s-trichrome staining (n = 4-6).
Cardiovascular Research, 2018, doi: doi.org/10.1093/cvr/cvy093. GW4064 purchased from Selleck.
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Effect of GE (Geniposide) on mRNA expressions of FXR and Nrf2 in HepG2 cells. GW4064 (5 μM) and t-BHQ (25 μM) were used as positive control, respectively.
RSC Adv, 2018, doi:10.1039/C8RA06345A. GW4064 purchased from Selleck.
Immunofluorescence staining of S1PR2 (×40).
IUBMB Life, 2016, 68(5):376-87. GW4064 purchased from Selleck.
Purity & Quality Control
Choose Selective FXR Inhibitors
Biological Activity
| Description | GW4064 is an agonist of farnesoid X receptor (FXR) with EC50 of 65 nM in CV1 cell line and displays no activity at other nuclear receptors at concentrations up to 1 μM. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| In vitro |
GW 4064 is a full agonist with EC50 values of 80 and 90 nM, respectively, in CV-1 cells transfected with mouse and human FXR expression vectors and an established reporter gene. There is no activity of GW 4064 on other nuclear receptors, including the retinoic acid receptor, at concentrations up to 1 μM. Thus, GW 4064 is a potent and selective nonsteroidal FXR agonist. [2] |
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| Cell Data |
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| Assay |
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| In vivo | Pharmacokinetic analysis in rats shows that GW 4064 possesses an oral bioavailability of 10% with a t1/2 = 3.5 h. Fisher rats are dosed with GW 4064 by oral gavage. After 7 days, a dose-dependent lowering of serum triglycerides is observed in the rats receiving GW 4064, with an ED50 = 20 mg/kg. [2] |
Protocol
| Animal Research: |
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Solubility (25°C)
| In vitro | DMSO | 100 mg/mL (184.21 mM) |
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| Water | Insoluble | |
| Ethanol | Insoluble | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 0.5% methylcellulose For best results, use promptly after mixing. |
11 mg/mL |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 542.84 |
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| Formula | C28H22Cl3NO4 |
| CAS No. | 278779-30-9 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
Bio Calculators
Molarity Calculator
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Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Molarity Calculator
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.
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