(E)-GW 4064
(E)-GW 4064 is a FXR agonist.
For research use only. We do not sell to patients.
- CAS No.: 1089660-72-9
- Formula: C28H22Cl3NO4
- Molecular Weight:542.84
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CV-1 | EC50 |
65 nM
Compound: 1a, GW-4064
|
Agonist activity at FXR expressed in african green monkey CV1 cells by luciferase reporter transient transfection assay
Agonist activity at FXR expressed in african green monkey CV1 cells by luciferase reporter transient transfection assay
|
[PMID: 18621523] |
| CV-1 | EC50 |
65 nM
Compound: 1a, GW-4064
|
Agonist activity at human FXR transfected in african green monkey CV1 cells by luciferase reporter gene transient transfection assay
Agonist activity at human FXR transfected in african green monkey CV1 cells by luciferase reporter gene transient transfection assay
|
[PMID: 19410460] |
| CV-1 | EC50 |
65 nM
Compound: 1, GW-4064
|
Increase in human FXR-mediated transient transcription of luciferase reporter gene transfected in african green monkey CV1 cells
Increase in human FXR-mediated transient transcription of luciferase reporter gene transfected in african green monkey CV1 cells
|
[PMID: 19586769] |
| CV-1 | EC50 |
65 nM
Compound: 1a, GW-4064
|
Agonist activity at human FXR LBD iexpressed in monkey CV-1 cells assessed as transactivation of luciferase reporter gene expression
Agonist activity at human FXR LBD iexpressed in monkey CV-1 cells assessed as transactivation of luciferase reporter gene expression
|
[PMID: 21256005] |
| CV-1 | EC50 |
65 nM
Compound: 1a, GW-4064
|
Agonist activity at human FXR LBD transfected in african green monkey CV1 cells after overnight incubation by luciferase reporter gene assay
Agonist activity at human FXR LBD transfected in african green monkey CV1 cells after overnight incubation by luciferase reporter gene assay
|
[PMID: 21890356] |
| CV-1 | EC50 |
65 nM
Compound: GW4064
|
Agonist activity at FXR (unknown origin) transfected into african green monkey CV1 cells assessed as ligand-mediated transcription by luciferase reporter/ transient transfection assay
Agonist activity at FXR (unknown origin) transfected into african green monkey CV1 cells assessed as ligand-mediated transcription by luciferase reporter/ transient transfection assay
|
[PMID: 25499883] |
| HEK293 | EC50 |
0.07 μM
Compound: GW-4064
|
Agonistic activity at FXR in HEK293 cells by GAL4 transactivation activity
Agonistic activity at FXR in HEK293 cells by GAL4 transactivation activity
|
[PMID: 17292610] |
| HEK293 | EC50 |
30 nM
Compound: GW-4064
|
Agonist activity at human full length FXR transfected in HEK293 cells coexpressing pTRexDest/pGL2promotor assessed as luciferase activity by direct reporter cellular assay
Agonist activity at human full length FXR transfected in HEK293 cells coexpressing pTRexDest/pGL2promotor assessed as luciferase activity by direct reporter cellular assay
|
[PMID: 20638278] |
| HEK293 | EC50 |
35 nM
Compound: GW-4064
|
Agonist activity at human GST-fused FXR LBD expressed in HEK293 cells coexpressing GAL4-DNA bindig domain and pFRluc by mammalian one-hybrid assay
Agonist activity at human GST-fused FXR LBD expressed in HEK293 cells coexpressing GAL4-DNA bindig domain and pFRluc by mammalian one-hybrid assay
|
[PMID: 20638278] |
| HEK293 | EC50 |
0.07 μM
Compound: 1, GW4064
|
Agonist activity at human recombinant FXR expressed in HEK293 cells coexpressing CMX-GAL4N by luciferase reporter gene assay
Agonist activity at human recombinant FXR expressed in HEK293 cells coexpressing CMX-GAL4N by luciferase reporter gene assay
|
[PMID: 22583617] |
| HEK293 | EC50 |
26 nM
Compound: GW4064
|
Agonist activity at human FXR expressed in HEK293 cells by luciferase reporter gene assay
Agonist activity at human FXR expressed in HEK293 cells by luciferase reporter gene assay
|
[PMID: 25305688] |
| HEK293 | EC50 |
373 nM
Compound: GW4064
|
Agonist activity at human FXR transfected in HEK293 cells assessed as transcriptional activity by luciferase reporter gene assay
Agonist activity at human FXR transfected in HEK293 cells assessed as transcriptional activity by luciferase reporter gene assay
|
[PMID: 26568144] |
| HEK293 | EC50 |
35 nM
Compound: 1; GW4064
|
Agonist activity at C-terminal Gal4-tagged human FXR (187 to 472 residues) expressed in HEK-293 cells co-expressing pFRluc by mammalian one hybrid assay
Agonist activity at C-terminal Gal4-tagged human FXR (187 to 472 residues) expressed in HEK-293 cells co-expressing pFRluc by mammalian one hybrid assay
|
[PMID: 27268696] |
| HEK-293T | EC50 |
95 nM
Compound: 2; GW4064
|
Agonist activity at human FXR expressed in HEK293T cells assessed as BSEP promoter driven cellular transcriptional activity after 24 hrs by luciferase reporter gene assay
Agonist activity at human FXR expressed in HEK293T cells assessed as BSEP promoter driven cellular transcriptional activity after 24 hrs by luciferase reporter gene assay
|
[PMID: 29148806] |
| HEK-293T | IC50 |
>10000 nM
Compound: 1; GW4064
|
Antagonist activity at human VDR transfected in HEK293T cells measured after 24 hrs by luciferase reporter gene assay
Antagonist activity at human VDR transfected in HEK293T cells measured after 24 hrs by luciferase reporter gene assay
|
[PMID: 32616182] |
| HEK-293T | EC50 |
0.09 μM
Compound: 3; GW4064
|
Activation of human FXR LBD expressed in HEK293T cells assessed as induction of receptor activation incubated for 12 to 14 hrs by luciferase reporter gene assay
Activation of human FXR LBD expressed in HEK293T cells assessed as induction of receptor activation incubated for 12 to 14 hrs by luciferase reporter gene assay
|
[PMID: 32687365] |
| HEK-293T | EC50 |
0.61 μM
Compound: 4; GW4064
|
Agonist activity at human farnesoid-X-receptor expressed in HEK293T cells co-expressing human RXRalpha assessed as receptor activation after 20 hrs by dual luciferase reporter assay
Agonist activity at human farnesoid-X-receptor expressed in HEK293T cells co-expressing human RXRalpha assessed as receptor activation after 20 hrs by dual luciferase reporter assay
|
10.1039/C5MD00149H |
| HeLa | EC50 |
0.51 μM
Compound: 3, GW4064
|
Agonist activity at human full length FXR expressed in HeLa cells cotransfected with pSG5-human RXR after 24 hrs by Dual-Glo luciferase reporter gene assay
Agonist activity at human full length FXR expressed in HeLa cells cotransfected with pSG5-human RXR after 24 hrs by Dual-Glo luciferase reporter gene assay
|
[PMID: 25934227] |
| HepG2 | EC50 |
0.02 μM
Compound: 3; GW4064
|
Transactivation of human FXR (unknown origin) expressed in HepG2 cells co-expressing pSG5RXR/pGL4.70 after 24 hrs post transfection by luciferase reporter gene assay
Transactivation of human FXR (unknown origin) expressed in HepG2 cells co-expressing pSG5RXR/pGL4.70 after 24 hrs post transfection by luciferase reporter gene assay
|
[PMID: 30996771] |
| Huh-7 | EC50 |
13.2 nM
Compound: 1; GW4064
|
Agonist activity at human FXR expressed in human HuH7 cells by luciferase reporter gene assay
Agonist activity at human FXR expressed in human HuH7 cells by luciferase reporter gene assay
|
[PMID: 32616182] |
Chemical Information
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CAS No. 1089660-72-9
-
Molecular Weight 542.84
-
Formula C28H22Cl3NO4
-
SMILES
ClC(C=C1OCC2=C(C(C)C)ON=C2C3=C(C=CC=C3Cl)Cl)=C(C=C1)/C=C/C4=CC(C(O)=O)=CC=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)