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CAS No.: 278779-30-9

GW 4064 Catalog No. CSN11129

Synonyms: GW4064

GW4064 is a selective, non-steroidal farnesoid X receptor (FXR) agonist (EC50 = 15 nM).

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Farnesoid X receptor (FXR) is a ligand-activated nuclear receptor regulating bile acid and lipid homeostasis. GW4064 is a synthetic agonist of FXR with an EC50 value of 65 nM in CV-1 cell lines. GW4064 also acts as a full agonist in CV-1 cells transfected with murine and human FXR expression vectors with EC50 values of 80 and 90 nM, respectively. No activity of GW4064 on other nuclear receptors were observed at concentrations up to 1 µM. GW4064 at 1 μM induced PGC-1α expression in HepG2 cells 24 hours after the treatment. GW4064 at the same concentration also increased the mRNA level of PGC-1α in L6, C2C12 myocytes and primary rat calvarial osteoblasts. The same treatment activated PGC-1α promoter and induced its expression in both FXR-nonexpressing and FXR-rich cells. GW4064 at 1 μM activated estrogen response (ER) element driven luciferase reporter in ER and FXR-null Cos-7 cells. Twenty-four hours after BALB/C mice received GW4064 (50 mg/kg body weight in gun acacia), the mRNA and protein levels of PGC-1α in both liver and skeletal muscles were significantly increased, together with elevated levels of SHP and decreased expression of CYP7A1, compared with vehicle-treated mice.
作用机制FXR has a structural conserved ligand-binding pocket with conformational flexibility to allow the binding of specific ligands. GW4064, as an FXR agonist, enters the FXR pocket and occupies a binding site to mediate the function of FXR.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
HEK293 cells	-	Function assay	-	Agonist activity at human FXR expressed in HEK293 cells by luciferase reporter gene assay, EC50=0.026 μM	25305688
HEK293 cells	-	Function assay	-	Agonistic activity at FXR in HEK293 cells by GAL4 transactivation activity, EC50=0.07 μM	17292610
HeLa cells	-	Function assay	24 h	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, EC50=0.51 μM	25934227

更多
动物研究
剂量
Mice: 20 mg/kg^[3] (i.p.), 50 mg/kg^[4] (i.p.); 2.5 mg/kg^[5] (i.v.); 150 mg/kg^[6] (p.o.)

给药途径
i.p., i.v., p.o.
参考文献

动物研究
剂量	Mice: 20 mg/kg^[3] (i.p.), 50 mg/kg^[4] (i.p.); 2.5 mg/kg^[5] (i.v.); 150 mg/kg^[6] (p.o.)
给药途径	i.p., i.v., p.o.

[1] Zhang S, Pan X, Jeong H. GW4064, an agonist of farnesoid X receptor, represses CYP3A4 expression in human hepatocytes by inducing small heterodimer partner expression. Drug Metab Dispos. 2015 May;43(5):743-8.
[2] Akwabi-Ameyaw A, Bass JY, et al.Conformationally constrained farnesoid X receptor (FXR) agonists: Naphthoic acid-based analogs of GW 4064. Bioorg Med Chem Lett, 2008, 18(15), 4339-4343.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.8422 mL
- 9.2109 mL
- 18.4217 mL
- 5 mM
- 0.3684 mL
- 1.8422 mL
- 3.6843 mL
- 10 mM
- 0.1842 mL
- 0.9211 mL
- 1.8422 mL

技术信息

CAS号

278779-30-9

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C28H22Cl3NO4

运输

蓝冰

分子量

542.84

别名

GW4064

溶解度

DMSO	500.0 mg/mL (921.1 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+40% PEG300+water	5 mg/mL	clear
PO	0.5% CMC-Na	38 mg/mL	suspension

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HEK293 cells	-	Function assay	-	Agonist activity at human FXR expressed in HEK293 cells by luciferase reporter gene assay, EC50=0.026 μM	25305688
HEK293 cells	-	Function assay	-	Agonistic activity at FXR in HEK293 cells by GAL4 transactivation activity, EC50=0.07 μM	17292610
HeLa cells	-	Function assay	24 h	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, EC50=0.51 μM	25934227
human Caco-2 cells	1 μM	Function assay	6 days	Activation of IBABP gene expression in human Caco-2 cells at 1 uM after 6 days by RT-PCR	17963371
human HepG2 cells	1 μM	Function assay	18 h	Decrease in CYP7A1 gene expression in human HepG2 cells at 1 uM after 18 hrs by RT-PCR	17963371
human HepG2 cells	1 μM	Function assay	18 h	Decrease in CYP7A1 gene expression in human HepG2 cells at 1 uM after 18 hrs by RT-PCR	17963371
human HepG2 cells	1 μM	Function assay	18 h	Activation of BSEP gene expression in human HepG2 cells at 1 uM after 18 hrs by RT-PCR	17963371
human Huh7 cells	1 μM	Function assay	18 h	Activation of SHP gene expression in human Huh7 cells at 1 uM after 18 hrs by RT-PCR	17963371
human Huh7 cells	1 μM	Function assay	18 h	Activation of BSEP gene expression in human Huh7 cells at 1 uM after 18 hrs by RT-PCR	17963371
monkey CV-1 cells	-	Function assay	-	Agonist activity at human FXR LBD iexpressed in monkey CV-1 cells assessed as transactivation of luciferase reporter gene expression, EC50=0.065 μM	21256005

GW 4064 Catalog No. CSN11129

靶点选择性

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