For research use only.

Catalog No.S2782

13 publications

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.

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10mM (1mL in DMSO) USD 150 In stock
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Selleck's GW4064 has been cited by 13 publications

4 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.

  • Myocardial infarct size and myocardial fibrosis were determined by Masson’s-trichrome staining (n = 4-6).

    Cardiovascular Research, 2018, doi: GW4064 purchased from Selleck.

  • 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

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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 M1mwS2Z2dmO2aX;uJIF{e2G7 MkLORYdwdmm|dDDhZ5Rqfmm2eTDheEBpfW2jbjDGXHIh\XiycnXzd4VlKGmwIFjFT|I6OyClZXzsd{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGVEPTB;MD6wNlYh|ryP NGX1ZWIzPTNyNU[4PC=>
monkey CV-1 cells NYnrbYE3TnWwY4Tpc44h[XO|YYm= MmPCRYdwdmm|dDDhZ5Rqfmm2eTDheEBpfW2jbjDGXHIhVEKGIHnlfJBz\XO|ZXSgbY4hdW:wa3X5JGNXNTFiY3XscJMh[XO|ZYPz[YQh[XNidILhcpNi[3SrdnH0bY9vKG:oIHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCneIDy[ZN{cW:wLDDFR|UxRTBwME[1JO69VQ>? NVXvdmpZOjF{NU[wNFU>
HEK293 cells Ml:2SpVv[3Srb36gZZN{[Xl? NHnBW4pC\2:waYP0bYMh[WO2aY\peJkh[XRiRmjSJIlvKEiHS{K5N{Bk\WyuczDifUBISUx2IITyZY5{[WO2aY\heIlwdiCjY4Tpeol1gSxiRVO1NF0xNjB5IN88US=> Mn;hNVczQTJ4MUC=
HeLa cells NHTQNHNHfW6ldHnvckBie3OjeR?= MlvTNlQhcA>? M2PsOGFod26rc4SgZYN1cX[rdImgZZQhcHWvYX6g[pVtdCCuZX7neIghTliUIHX4dJJme3OnZDDpckBJ\UyjIHPlcIx{KGOxdILhcpNn\WO2ZXSge4l1cCCyU1e1MYh2dWGwIGLYVkBi\nSncjCyOEBpenNiYomgSJVidC2JbH:gcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCHQ{WwQVAvPTFizszN MnHKNlU6OzR{Mke=
human Caco-2 cells MnfUSpVv[3Srb36gZZN{[Xl? M4PsbVEh|ryP MmrLOkBl[Xm| MlzkRYN1cX[jdHnvckBw\iCLQlHCVEBo\W6nIHX4dJJme3Orb36gbY4hcHWvYX6gR4Fkdy1{IHPlcIx{KGG2IEGgeW0h[W[2ZYKgOkBl[Xm|IHL5JHJVNVCFUh?= M2LicFE4QTZ|M{ex
human HepG2 cells MkHESpVv[3Srb36gZZN{[Xl? NFLyfGsyKM7:TR?= MVKxPEBp MmrmSIVkemWjc3WgbY4hS1mSN1GxJIdmdmViZYjwdoV{e2mxbjDpckBpfW2jbjDI[ZBIOiClZXzsd{BifCBzIIXNJIFnfGW{IEG4JIhzeyCkeTDSWE1RS1J? M4fYNFE4QTZ|M{ex
human HepG2 cells MmXlSpVv[3Srb36gZZN{[Xl? M2DHS|Eh|ryP M3jGW|E5KGh? NXi4dIZKTGWlcnXhd4UhcW5iQ2nQO2EyKGenbnWg[ZhxemW|c3nvckBqdiCqdX3hckBJ\XCJMjDj[YxteyCjdDCxJJVOKGGodHXyJFE5KGi{czDifUBTXC2SQ2K= NFrUeJoyPzl4M{O3NS=>
human Huh7 cells MVLGeY5kfGmxbjDhd5NigQ>? NFj5Z5QyKM7:TR?= MlnPNVghcA>? MnjJRYN1cX[jdHnvckBw\iCVSGCg[4Vv\SCneIDy[ZN{cW:wIHnuJIh2dWGwIFj1bFch[2WubIOgZZQhOSC3TTDh[pRmeiBzODDodpMh[nliUmStVGNT M3zKRlE4QTZ|M{ex
human HepG2 cells MWHGeY5kfGmxbjDhd5NigQ>? NVX5[GZ1OSEQvF2= M1LkeFE5KGh? M371RmFkfGm4YYTpc44hd2ZiQmPFVEBo\W6nIHX4dJJme3Orb36gbY4hcHWvYX6gTIVxTzJiY3XscJMh[XRiMTD1UUBi\nSncjCxPEBpenNiYomgVnQuWEOU NYrWNpNWOTd7NkOzO|E>
human Huh7 cells M{XpR2Z2dmO2aX;uJIF{e2G7 NI\ieVUyKM7:TR?= NEXxS2QyQCCq NF:2W49C[3SrdnH0bY9vKG:oIFLTSXAh\2WwZTDlfJBz\XO|aX;uJIlvKGi3bXHuJGh2cDdiY3XscJMh[XRiMTD1UUBi\nSncjCxPEBpenNiYomgVnQuWEOU MWKxO|k3OzN5MR?=

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
PTEN / p-AKT / AKT ; 

PubMed: 25187826     

Protein expression levels of PTEN, phosphorylated and total Akt in LNcaP cells treated with a vehicle control (DMSO), CDCA or GW4064. 

p-EGFR / EGFR / p-ERK / ERK / p-Src / Src ; 

PubMed: 23119029     

A. Time-course and dose-response for GW4064-induced inhibition of EGFR (Tyr845) phosphorylation. B. Time-course and dose-response for GW4064-induced inhibition of ERK1/2 phosphorylation. C. Time-course and dose-response for GW4064-induced inhibition of Src (Tyr 416) phosphorylation. Phosphorylation of EGFR (Tyr845), ERK1/2 and Src (Tyr 416) was determined by immunoblotting with anti-phospho-EGFR (Tyr845), anti-phospho-ERK1/2 and anti-phospho-Src (Tyr 416) antibody, respectively. For time-course experiments, SNU-C4 cells were treated with 1 µM GW4064 for the indicated times at 37°C. For dose-response experiments, cells were treated with the indicated concentrations of GW4064 for 20 min at 37°C. Immunoblotting for total EGFR, ERK2 or Src was used as a loading control. Immunoblots are representative of at least 3 separate experiments. Numbers between immunoblots represent densitometry. Experimental/control ratios were calculated after normalizing each test band to the respective EGFR, ERK2 or Src band.

SOCS3 / p21 / p-STAT3 / STAT3 ; 

PubMed: 26416445     

HepG2 cells and Huh7 cells were treated with GW4064 (2 μM) or vehicle DMSO for 24 h. The protein levels of SOCS3, p21, total STAT3 (t-SATA3) and phosphoraylated STAT3 (p-STAT3) were assayed by Western blot, taking GAPDH as a loading control

25187826 23119029 26416445
Growth inhibition assay
Cell proliferation ; 

PubMed: 25187826     

LNcaP cells were treated with CDCA (5 μM), GW4064 (2 μM) or vehicle control (DMSO) and cell proliferation ability was measured using BrdU assays. A450 absorption was assayed following treatment for 24 h. 

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:


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  • Animal Models: Fisher rats
  • 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
Smiles CC(C)C1=C(COC2=CC(=C(C=C2)/C=C/C3=CC=CC(=C3)C(O)=O)Cl)C(=NO1)C4=C(Cl)C=CC=C4Cl

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Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
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% DMSO % % Tween 80 % ddH2O

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID