GW4064

製品コード：S2782 純度：99.80%

GW4064 is an agonist of farnesoid X receptor (FXR) with EC50 of 65 nM in CV1 cell line and displays no activity at other nuclear receptors at concentrations up to 1 μM. GW4064 stimulates autophagy in MCF-7 cells.

CAS No. 278779-30-9

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
5mg	JPY 22000	国内在庫あり
25mg	JPY 55500	国内在庫あり
1g	JPY 435000	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

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製品安全説明書

現在のバッチを見る：純度： 99.80%

99.80

GW4064関連製品

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FXR阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
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

製品説明

Targets

FXR ^[1]
(CV1)

65 nM(EC50)

In Vitro
In vitro	GW 4064 is a full agonist with EC50 values of 80 and 90 nM, respectively, in CV-1 cells transfected with mouse and human FXR expression vectors and an established reporter gene. There is no activity of GW 4064 on other nuclear receptors, including the retinoic acid receptor, at concentrations up to 1 μM. Thus, GW 4064 is a potent and selective nonsteroidal FXR agonist. ^[2]
Kinase Assay	FXR Transient Transfection Assay
Kinase Assay	CV1 cells are maintained in DMEM high glucose medium. The CV1 cells are harvested 72 hours before transfection and plated in DMEM-F12 phenol red free medium containing 5% charcoal/dextran treated fetal bovine serum and 2 mM glutamine. On the day of transfection, the CV1 cells are harvested in DMEM-F12 phenol red free medium containing 5% charcoal/dextran treated fetal bovine serum and 2 mM glutamine, counted and seeded into a T-175 cm² flask at a density of 14 million cells per flask before adding the transfection mix. The FuGENE® 6 transfection mix containing 0.55 μg pFA-CMV-GAL4-human FXR LBD expression plasmid, 10.92 μg of the (UAS)-tk-Luciferase reporter plasmid, 20.75 μg of pBluescript II KS+, and 3.82 μg of a human steroid receptor co-activator (SRC-1) construct is incubated and then added to the CV1 cells for overnight incubation in incubator. The transfected CV1 cells are harvested in DMEM-F12 phenol red free medium containing 5% charcoal/dextran treated fetal bovine serum and 2 mM glutamine. Transfected cells are added at a concentration of 3750 cells/well to 384-well plates containing ligands. Luciferase expression is measured using Steady-Glo?Luciferase Assay System 24 hr after incubation with ligand. GW4064X is used as the control, and data are normalized to GW4064X as % control.
細胞実験	細胞株	HepG2 cells
	濃度	10 µM
	反応時間	2 h
	実験の流れ	Cells were treated with indicated concentration of drug for 2 h.
実験結果図	Methods	Biomarkers	結果図	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

In Vivo
In Vivo	Pharmacokinetic analysis in rats shows that GW 4064 possesses an oral bioavailability of 10% with a t_1/2 = 3.5 h. Fisher rats are dosed with GW 4064 by oral gavage. After 7 days, a dose-dependent lowering of serum triglycerides is observed in the rats receiving GW 4064, with an ED50 = 20 mg/kg. ^[2]
動物実験	動物モデル	Fisher rats
	投与量	0-100 mg/kg
	投与経路	Orally, b.i.d.

参考
[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

化学情報

分子量	542.84	化学式	C₂₈H₂₂Cl₃NO₄
CAS No.	278779-30-9	SDF	Download GW4064 SDFをダウンロードする
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
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (184.21 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo Batch: Add solvents to the product individually and in order.					投与溶液組成計算機
	Clear solution	5% DMSO 1 95% Corn oil	0.6mg/ml (1.11mM)	Taking the 1 mL working solution as an example, add 50 μL of 12 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.	投与溶液組成計算機
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	2.5mg/ml (4.61mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	0.5% methylcellulose	10.0mg/ml (18.42mM)	Taking the 1 mL working solution as an example, take 10 mg of this product, add it to 1 ml of 0.5% methylcellulose clear solution, and mix evenly to form a uniform suspension. The mixed solution should be used immediately for optimal results.

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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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):
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