GW4064

目錄號：S2782 Purity: 99.80%

GW4064是一種farnesoid X receptor (FXR)激動劑，CV1細胞系中EC50為65 nM。濃度達到1 μM時，對其他核受體沒有活性。GW4064在MCF-7細胞中可刺激自噬。

GW4064 Chemical Structure

CAS: 278779-30-9

規(guī)格	價格	庫存
10mM (1mL in DMSO)	790	現(xiàn)貨
5mg	571.57	現(xiàn)貨
25mg	2220.65	現(xiàn)貨
50mg	3013.36	現(xiàn)貨
1g	23751	現(xiàn)貨
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產(chǎn)品質(zhì)控

批次：純度： 99.80%

99.80

GW4064相關產(chǎn)品

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細胞實驗數(shù)據(jù)示例

細胞系	實驗類型	給藥濃度	孵育時間	活性描述	文獻信息
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
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生物活性

產(chǎn)品描述

GW4064是一種farnesoid X receptor (FXR)激動劑，CV1細胞系中EC50為65 nM。濃度達到1 μM時，對其他核受體沒有活性。GW4064在MCF-7細胞中可刺激自噬。

靶點

FXR ^[1]
(CV1)

65 nM(EC50)

體外研究(In Vitro)
體外研究活性	GW 4064是一種完全激動劑，在轉染有鼠源和人源FXR表達載體以及確定的報告基因的CV-1細胞中， EC50分別為80和90。GW 4064直到1 μM濃度對其它核受體也沒有活性，包括維甲酸受體。因此, GW 4064是一種強有效和選擇性的非類固醇FXR激動劑^[2]。
實驗圖片	檢測方法	檢測指標	實驗圖片	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

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	大鼠體內(nèi)藥代動力學實驗顯示GW 4064口服生物利用度為10%，t_1/2 = 3.5小時。 Fisher大鼠按劑量填喂給藥。7天之后, GW 4064處理的大鼠血清甘油三酯下降并具有劑量依賴特性，ED50 = 20 mg/kg^[2]。
動物實驗	Animal Models	Fisher大鼠
	Dosages	0-100 mg/kg
	Administration	口服, 一天兩次

參考文獻
[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.

參考文獻

[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.

化學信息&溶解度

分子量	542.84	分子式	C₂₈H₂₂Cl₃NO₄
CAS號	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
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1年-80°C溶于溶劑
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1個月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 100 mg/mL ( (184.21 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 100 mg/mL ( (184.21 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 100 mg/mL ( (184.21 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 100 mg/mL ( (184.21 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計算器

體內(nèi)溶解度批次：現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑					動物體內(nèi)配方計算器
體內(nèi)溶解度批次：現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑	澄清溶液	5% DMSO 1 95% Corn oil	0.6mg/ml (1.11mM)	以1 mL工作液為例，取50μL 12mg/ml的澄清DMSO儲備液加到950μL玉米油中，混合均勻。工作液請現(xiàn)配現(xiàn)用！	動物體內(nèi)配方計算器
澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	2.5mg/ml (4.61mM)	以 1 mL 工作液為例,取50μL50mg/ml的澄清DMSO儲備液加到400μLPEG300中,混合均勻使其澄清;向上述體系中加入50μLTween80,混合均勻使其澄清;然后繼續(xù)加入500μLddH2O定容至1mL。工作液請現(xiàn)配現(xiàn)用!
均勻懸濁液	0.5% methylcellulose	10.0mg/ml (18.42mM)	以1 mL工作液為例，取10 mg此產(chǎn)品，加入到1ml的0.5% methylcellulose澄清溶液，混合均勻使其成為均勻懸濁液。工作液請現(xiàn)配現(xiàn)用！

實驗計算

摩爾濃度計算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計算器分子量計算器

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

給藥劑量 mg/kg 動物平均體重 g 每只動物給藥體積 μL 動物數(shù)量只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計算結果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

技術支持

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操作手冊

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C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

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GW4064

產(chǎn)品質(zhì)控

GW4064相關產(chǎn)品

細胞實驗數(shù)據(jù)示例

生物活性

化學信息&溶解度

實驗計算

技術支持