Catalog No.S2782

GW4064 Chemical Structure

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.

Size Price Stock Quantity  
In DMSO USD 150 In stock
USD 70 In stock
USD 110 In stock
USD 270 In stock
USD 370 In stock
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2 Customer Reviews

  • 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.

    Immunofluorescence staining of S1PR2 (×40).

    IUBMB Life, 2016, 68(5):376-87. GW4064 purchased from Selleck.

Purity & Quality Control

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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.
FXR [1]
65 nM(EC50)
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293 cells MVHGeY5kfGmxbjDhd5NigQ>? Mni3RYdwdmm|dDDhZ5Rqfmm2eTDheEBpfW2jbjDGXHIh\XiycnXzd4VlKGmwIFjFT|I6OyClZXzsd{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGVEPTB;MD6wNlYh|ryP M4HTV|I2OzB3Nki4
monkey CV-1 cells NEjnV5NHfW6ldHnvckBie3OjeR?= MmryRYdwdmm|dDDhZ5Rqfmm2eTDheEBpfW2jbjDGXHIhVEKGIHnlfJBz\XO|ZXSgbY4hdW:wa3X5JGNXNTFiY3XscJMh[XO|ZYPz[YQh[XNidILhcpNi[3SrdnH0bY9vKG:oIHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCneIDy[ZN{cW:wLDDFR|UxRTBwME[1JO69VQ>? NUXnSYFPOjF{NU[wNFU>
HEK293 cells MYDGeY5kfGmxbjDhd5NigQ>? MYnB[49vcXO2aXOgZYN1cX[rdImgZZQhTliUIHnuJGhGUzJ7MzDj[YxteyCkeTDHRWw1KHS{YX7zZYN1cX[jdHnvckBi[3Srdnn0fUwhTUN3ME2wMlA4KM7:TR?= MV6xO|I6OjZzMB?=
HeLa cells NWr6NpgyTnWwY4Tpc44h[XO|YYm= Mly1NlQhcA>? NY\5WFFXSWexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBnfWyuIHzlcod1cCCIWGKg[ZhxemW|c3XkJIlvKEinTHGgZ4VtdHNiY3;0doFve2[nY4Tl[EB4cXSqIIDTS|UucHWvYX6gVnhTKGGodHXyJFI1KGi{czDifUBFfWGuLVfsc{BtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFXDOVA:OC53MTFOwG0> MkftNlU6OzR{Mke=
human Caco-2 cells MU\GeY5kfGmxbjDhd5NigQ>? NWr5ZY4{OSEQvF2= M4LV[lYh\GG7cx?= NF\EO3JC[3SrdnH0bY9vKG:oIFnCRWJRKGenbnWg[ZhxemW|c3nvckBqdiCqdX3hckBE[WOxLUKgZ4VtdHNiYYSgNUB2VSCjZoTldkA3KGSjeYOgZpkhWlRvUFPS NYDiVVhoOTd7NkOzO|E>
human HepG2 cells NYPXTohSTnWwY4Tpc44h[XO|YYm= M1T2TVEh|ryP MWWxPEBp M2jwcWRm[3KnYYPlJIlvKEO\UEfBNUBo\W6nIHX4dJJme3Orb36gbY4hcHWvYX6gTIVxTzJiY3XscJMh[XRiMTD1UUBi\nSncjCxPEBpenNiYomgVnQuWEOU M{HnfFE4QTZ|M{ex
human HepG2 cells MorESpVv[3Srb36gZZN{[Xl? NWThPY5OOSEQvF2= MnG2NVghcA>? NHm2cFZF\WO{ZXHz[UBqdiCFWWC3RVEh\2WwZTDlfJBz\XO|aX;uJIlvKGi3bXHuJGhmeEd{IHPlcIx{KGG2IEGgeW0h[W[2ZYKgNVghcHK|IHL5JHJVNVCFUh?= M3n5blE4QTZ|M{ex
human Huh7 cells MXjGeY5kfGmxbjDhd5NigQ>? NF;tXVIyKM7:TR?= MmX2NVghcA>? NXvsZlN1SWO2aY\heIlwdiCxZjDTTHAh\2WwZTDlfJBz\XO|aX;uJIlvKGi3bXHuJGh2cDdiY3XscJMh[XRiMTD1UUBi\nSncjCxPEBpenNiYomgVnQuWEOU M{XKOVE4QTZ|M{ex
human HepG2 cells MlPkSpVv[3Srb36gZZN{[Xl? NXqxb3R4OSEQvF2= MWSxPEBp NVq1cFBkSWO2aY\heIlwdiCxZjDCV2VRKGenbnWg[ZhxemW|c3nvckBqdiCqdX3hckBJ\XCJMjDj[YxteyCjdDCxJJVOKGGodHXyJFE5KGi{czDifUBTXC2SQ2K= NVLQc|MxOTd7NkOzO|E>
human Huh7 cells MYHGeY5kfGmxbjDhd5NigQ>? MWKxJO69VQ>? MVWxPEBp MnXuRYN1cX[jdHnvckBw\iCEU1XQJIdmdmViZYjwdoV{e2mxbjDpckBpfW2jbjDIeYg4KGOnbHzzJIF1KDFidV2gZYZ1\XJiMUigbJJ{KGK7IGLUMXBEWg>? M2\jcFE4QTZ|M{ex

... Click to View More Cell Line Experimental Data

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]


Animal Research:


+ Expand
  • Animal Models: Fisher rats
  • Formulation: 0.5% methyl cellulose
  • Dosages: 0-100 mg/kg
  • Administration: Orally, b.i.d.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (184.21 mM)
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


CAS No. 278779-30-9
Storage powder
in solvent
Synonyms N/A

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID