(E)-GW 4064

目录号: HY-50108A: FAQs
Data Sheet 产品使用指南

摩尔计算器

(E)-GW 4064 是 FXR 的激动剂。

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(E)-GW 4064 Chemical Structure

CAS No. : 1089660-72-9

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生物活性
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参考文献

生物活性

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

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
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]
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: 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]
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	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	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	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: 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]
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	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]
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
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]
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]

分子量

542.84

Formula

C₂₈H₂₂Cl₃NO₄

CAS 号

1089660-72-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料

产品使用指南 (1538 KB)

参考文献

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

(E)-GW 4064 相关分类

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摩尔计算器
稀释计算器

The molarity calculator equation

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

质量		浓度		体积		分子量 *
	=		×		×

The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)	×	体积 _(start)	=	浓度 _(final)	×	体积 _(final)
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

(E)-GW 40641089660-72-9FXRNR1H4Inhibitorinhibitorinhibit

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营业执照（三证合一）

(E)-GW 4064

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