GW4064

目录号：S2782 Purity: 99.80%

GW4064是一种farnesoid X receptor (FXR)激动剂，CV1细胞系中EC50为65 nM。浓度达到1 μM时，对其他核受体没有活性。GW4064在MCF-7细胞中可刺激自噬。

GW4064 Chemical Structure

CAS: 278779-30-9

规格	价格	库存
10mM (1mL in DMSO)	790	现货
5mg	571.57	现货
25mg	2220.65	现货
50mg	3013.36	现货
1g	23751	现货
更大包装有超大折扣
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产品质控

批次：纯度： 99.80%

99.80

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细胞实验数据示例

细胞系	实验类型	给药浓度	孵育时间	活性描述	文献信息
HepG2	Function assay	1 uM	18 hrs	Decrease in CYP7A1 gene expression in human HepG2 cells at 1 uM after 18 hrs by RT-PCR	17963371
Caco-2	Function assay	1 uM	6 days	Activation of IBABP gene expression in human Caco-2 cells at 1 uM after 6 days by RT-PCR	17963371
HepG2	Function assay	1 uM	18 hrs	Activation of BSEP gene expression in human HepG2 cells at 1 uM after 18 hrs by RT-PCR	17963371
Huh7	Function assay	1 uM	18 hrs	Activation of SHP gene expression in human Huh7 cells at 1 uM after 18 hrs by RT-PCR	17963371
Huh7	Function assay	1 uM	18 hrs	Activation of BSEP gene expression in human Huh7 cells at 1 uM after 18 hrs by RT-PCR	17963371
HepG2	Function assay	10 uM	10 mins	Induction of FXR-mediated Akt-phosphorylation at S473 site in serum-starved human HepG2 cells at 10 uM measured after 10 mins by western blot analysis	27372840
HepG2	Function assay	10 uM	10 mins	Induction of FXR-mediated Akt-phosphorylation in serum-starved human HepG2 cells assessed as increase in GSK-3beta-phosphorylation at 10 uM measured after 10 mins by western blot analysis	27372840
HepG2	Function assay	10 uM		Induction of FXR-mediated SHP mRNA expression in serum-starved human HepG2 cells at 10 uM measured after overnight incubation by qPCR analysis	27372840
HepG2	Function assay	10 uM		Activation of FXR in human HepG2 cells assessed as upregulation of SHP mRNA expression at 10 uM by RT-PCR method	30031618
HepG2	Function assay	10 uM		Activation of FXR in human HepG2 cells assessed as upregulation of FXR mRNA expression at 10 uM by RT-PCR method	30031618
HepG2	Function assay	10 uM		Activation of FXR in human HepG2 cells assessed as downregulation of SREBP-1c mRNA expression at 10 uM by RT-PCR method	30031618
3T3L1	Function assay	10 uM		Reduction in lipid accumulation in mouse 3T3L1 cells at 10 uM by Oil Red O staining-based absorbance method relative to control	30342957
HeLa	Function assay		24 hrs	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
insect cells	Function assay		1 hr	Agonist activity at recombinant human GST-tagged FXR ligand binding domain (193 to 472 residues) expressed in baculovirus infected insect cells assessed as induction of interaction with biotin labelled SRC-1 after 1 hr by HTRF assay, EC50 = 0.019 μM.	29148806
HEK293T	Function assay		24 hrs	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, EC50 = 0.095 μM.	29148806
HEK293	Function 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, EC50 = 0.035 μM.	20638278
HEK293	Function assay			Agonist activity at human full length FXR transfected in HEK293 cells coexpressing pTRexDest/pGL2promotor assessed as luciferase activity by direct reporter cellular assay, EC50 = 0.03 μM.	20638278
CV1	Function assay			Increase in human FXR-mediated transient transcription of luciferase reporter gene transfected in african green monkey CV1 cells, EC50 = 0.065 μM.	19586769
CV1	Function assay			Agonist activity at human FXR transfected in african green monkey CV1 cells by luciferase reporter gene transient transfection assay, EC50 = 0.065 μM.	19410460
CV1	Function assay			Agonist activity at FXR expressed in african green monkey CV1 cells by luciferase reporter transient transfection assay, EC50 = 0.065 μM.	18621523
HEK293	Function assay			Agonistic activity at FXR in HEK293 cells by GAL4 transactivation activity, EC50 = 0.07 μM.	17292610
CV-1	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
CV1	Function assay			Agonist activity at human FXR LBD transfected in african green monkey CV1 cells after overnight incubation by luciferase reporter gene assay, EC50 = 0.065 μM.	21890356
HEK293	Function assay			Agonist activity at human recombinant FXR expressed in HEK293 cells coexpressing CMX-GAL4N by luciferase reporter gene assay, EC50 = 0.07 μM.	22583617
HEK293	Function assay			Agonist activity at human FXR expressed in HEK293 cells by luciferase reporter gene assay, EC50 = 0.026 μM.	25305688
CV1	Function 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, EC50 = 0.065 μM.	25499883
HEK293	Function assay			Agonist activity at human FXR transfected in HEK293 cells assessed as transcriptional activity by luciferase reporter gene assay, EC50 = 0.373 μM.	26568144
HEK-293	Function 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, EC50 = 0.035 μM.	27268696
点击查看更多细胞系数据

生物活性

产品描述

GW4064是一种farnesoid X receptor (FXR)激动剂，CV1细胞系中EC50为65 nM。浓度达到1 μM时，对其他核受体没有活性。GW4064在MCF-7细胞中可刺激自噬。

靶点

FXR ^[1]
(CV1)

65 nM(EC50)

体外研究(In Vitro)
体外研究活性	GW 4064是一种完全激动剂，在转染有鼠源和人源FXR表达载体以及确定的报告基因的CV-1细胞中， EC50分别为80和90。GW 4064直到1 μM浓度对其它核受体也没有活性，包括维甲酸受体。因此, GW 4064是一种强有效和选择性的非类固醇FXR激动剂^[2]。
实验图片	检测方法	检测指标	实验图片	PMID
	Western blot	PTEN / p-AKT / AKT p-EGFR / EGFR / p-ERK / ERK / p-Src / Src SOCS3 / p21 / p-STAT3 / STAT3		25187826
	Growth inhibition assay	Cell proliferation		25187826

体内研究(In Vivo)
体内研究活性	大鼠体内药代动力学实验显示GW 4064口服生物利用度为10%，t_1/2 = 3.5小时。 Fisher大鼠按剂量填喂给药。7天之后, GW 4064处理的大鼠血清甘油三酯下降并具有剂量依赖特性，ED50 = 20 mg/kg^[2]。
动物实验	Animal Models	Fisher大鼠
	Dosages	0-100 mg/kg
	Administration	口服, 一天两次

参考文献
[1] Akwabi-Ameyaw A et al., Bioorg Med Chem Lett, 2008, 18(15), 4339-4343. [2] Maloney PR, et al., J Med Chem, 2000, 43(16), 2971-2974. [3] Wang LJ, et al. Nutrients. 2022 Aug 2;14(15):3176.

参考文献

化学信息&溶解度

分子量	542.84	分子式	C₂₈H₂₂Cl₃NO₄
CAS号	278779-30-9	SDF	Download GW4064 SDF
Smiles	CC(C)C1=C(C(=NO1)C2=C(C=CC=C2Cl)Cl)COC3=CC(=C(C=C3)C=CC4=CC(=CC=C4)C(=O)O)Cl
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

DMSO : 100 mg/mL ( (184.21 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 100 mg/mL ( (184.21 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 100 mg/mL ( (184.21 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 100 mg/mL ( (184.21 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度批次：现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂					动物体内配方计算器
体内溶解度批次：现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂	澄清溶液	5% DMSO 1 95% Corn oil	0.6mg/ml (1.11mM)	以1 mL工作液为例，取50μL 12mg/ml的澄清DMSO储备液加到950μL玉米油中，混合均匀。工作液请现配现用！	动物体内配方计算器
澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	2.5mg/ml (4.61mM)	以 1 mL 工作液为例,取50μL50mg/ml的澄清DMSO储备液加到400μLPEG300中,混合均匀使其澄清;向上述体系中加入50μLTween80,混合均匀使其澄清;然后继续加入500μLddH2O定容至1mL。工作液请现配现用!
均匀悬浊液	0.5% methylcellulose	10.0mg/ml (18.42mM)	以1 mL工作液为例，取10 mg此产品，加入到1ml的0.5% methylcellulose澄清溶液，混合均匀使其成为均匀悬浊液。工作液请现配现用！

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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