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Cat. No.: HY-50108A

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(E)-GW 4064

(E)-GW 4064 is a FXR agonist.

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CAS No.: 1089660-72-9
Formule: C₂₈H₂₂Cl₃NO₄
Masse moléculaire:542.84

Stockage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (267 KB)

(E)-GW 4064 Chemical Structure

CAS No.: 1089660-72-9

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- Cellular Effect
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

(E)-GW 4064 is a FXR agonist^[1].

Cellular Effect

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

CAS No. 1089660-72-9
Masse moléculaire 542.84
Formule 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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (267 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Helen B. Hartman, et al. FXR Agonists for the Treatment of Malignancies. Patent US20080299118.

Calculators

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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