GW 4064

Name: GW 4064
Brand: MedChemExpress
SKU: HY-50108
Rating: 5.0 (56 reviews)

Cat. No.: HY-50108 Purity: 99.79%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

GW 4064 is a potent FXR agonist with an EC₅₀ of 65 nM.

For research use only. We do not sell to patients.

CAS No. : 278779-30-9

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	In-stock	Estimated Time of Arrival: December 31
500 mg	Get quote
1 g	Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 56 publication(s) in Google Scholar

Other Forms of GW 4064:

(E)-GW 4064 Get quote

56 Publications Citing Use of MCE GW 4064

RT-PCR

: GW 4064 purchased from MedChemExpress. Usage Cited in: J Transl Med. 2019 Dec 13;17(1):418. [Abstract]; FXR suppresses gluconeogenesis and enhances glucose uptake in the HK-2 cell lines. The protein expression of FXR is obviously upregulates by GW4064 at 24, 48 and 72 h in the HK-2 cell lines.

: GW 4064 purchased from MedChemExpress. Usage Cited in: J Transl Med. 2019 Dec 13;17(1):418. [Abstract]; FXR suppresses gluconeogenesis and enhances glucose uptake in the HK-2 cell lines. GW4064 at 4 μM inhibits the mRNA level of FXR.

: GW 4064 purchased from MedChemExpress. Usage Cited in: FASEB J. 2019 Feb;33(2):2472-2483. [Abstract]; FXRa protein expression in nontransduced (treated with DMSO or GW4064 for 9 d) and transduced shFXRa-dHepaRG cells, by Western blot analysis.

: GW 4064 purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2018 Jun 28;19(7). pii: E1898. [Abstract]; Western blotting for p-FAK and total FAK. Cells are treated with vehicle control (Cont), 10 μM GW4064, or 32 μM GS in the absence or presence of 10 ng/mL TGF-β for 48 h. .

: GW 4064 purchased from MedChemExpress. Usage Cited in: FEBS Lett. 2017 Sep;591(18):2836-2847. [Abstract]; GW4064 inhibits NLRP3 inflammasome activation. The human PBMCs are primed with 500 ng/mL LPS for 3 h followed by GW4064 of indicated concentration(s) and different second signal stimulations, including Nigericin. The protein levels of activated caspase-1 and cleaved IL-1b are detected by western blot.

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

GW 4064 is a potent FXR agonist with an EC₅₀ of 65 nM.

IC₅₀ & Target

EC50: 65 nM (FXR)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
CV-1	EC₅₀	65 nM Compound: 1, GW-4064	Increase in human FXR-mediated transient transcription of luciferase reporter gene transfected in african green monkey CV1 cells Increase in human FXR-mediated transient transcription of luciferase reporter gene transfected in african green monkey CV1 cells	[PMID: 19586769]
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]
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 human FXR LBD iexpressed in monkey CV-1 cells assessed as transactivation of luciferase reporter gene expression Agonist activity at human FXR LBD iexpressed in monkey CV-1 cells assessed as transactivation of luciferase reporter gene expression	[PMID: 21256005]
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]
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]
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]
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]
HT-29	IC₅₀	13.8 μM Compound: 74; GW4064	Antiproliferative activity against human HT-29 cells incubated for 48 hrs by CCK-8 method Antiproliferative activity against human HT-29 cells incubated for 48 hrs by CCK-8 method	[PMID: 38142509]
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]
SW-620	IC₅₀	7.6 μM Compound: 74; GW4064	Antiproliferative activity against human SW620 cells incubated for 48 hrs by CCK-8 method Antiproliferative activity against human SW620 cells incubated for 48 hrs by CCK-8 method	[PMID: 38142509]

In Vitro

Treatment with different concentrations of GW4064 (1, 2.5, 5, 10 μM) reduces the lipid accumulation in the cells. Concordantly, GW4064 treatment significantly represses oleic acid-induced CD36 protein levels in a dose-dependent manner. Taken together, these data indicate that prevention of hepatic lipid accumulation is likely due to an inhibition of Cd36 expression by long-term GW4064 treatment^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

GW4064 suppresses weight gain in C57BL/6 mice fed with either a high-fat diet (HFD) or high-fat, high-cholesterol diet. GW4064 treatment of mice on HFD significantly represses diet-induced hepatic steatosis as evidenced by lower triglyceride and free fatty acid level in the liver. GW4064 markedly reduces lipid transporter CD36 expression without affecting expression of genes that are directly involved in lipogenesis. GW4064 treatment attenuates hepatic inflammation while having no effect on white adipose tissue^[2]. GW4064 (30 mg/kg) treatment results in substantial, statistically significant reductions in serum activities of ALT, AST, LDH, and ALP in the ANIT-treated rats. Serum bile acid levels are also significantly reduced by GW4064 treatment. Bilirubin levels are decreased in the GW4064-treated rats, but statistical significance is not achieved. Notably, GW4064 is much more effective in decreasing these markers of liver damage than TUDCA, which reduces only LDH levels^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

542.84

Formula

C₂₈H₂₂Cl₃NO₄

CAS No.

278779-30-9

Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=CC(/C=C/C2=CC=C(C=C2Cl)OCC3=C(ON=C3C4=C(Cl)C=CC=C4Cl)C(C)C)=C1)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (184.22 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

DMF : 100 mg/mL (184.22 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.8422 mL	9.2108 mL	18.4216 mL
5 mM	0.3684 mL	1.8422 mL	3.6843 mL
10 mM	0.1842 mL	0.9211 mL	1.8422 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.61 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMF 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.61 mM); Clear solution
Protocol 3

Add each solvent one by one: 10% DMF 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.61 mM); Clear solution
Protocol 4

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.83 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 5 mg/mL (9.21 mM); Suspended solution; Need ultrasonic
Protocol 2

Add each solvent one by one: 0.5% CMC/saline water
Solubility: 5 mg/mL (9.21 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.79%

Select Batch:

Data Sheet (281 KB) SDS (393 KB)

COA (252 KB) HNMR (305 KB) RP-HPLC (267 KB) MS (239 KB) Elemental Analysis Report (110 KB)

Handling Instructions (2659 KB)

References

[1]. Akwabi-Ameyaw A, 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. [Content Brief]

[2]. Ma Y, et al. Synthetic FXR agonist GW4064 prevents diet-induced hepatic steatosis and resistance. Pharm Res. 2013 May;30(5):1447-57. [Content Brief]

[3]. Liu Y, et al. Hepatoprotection by the farnesoid X receptor agonist GW4064 in rat models of intra- and extrahepatic cholestasis. J Clin Invest. 2003 Dec;112(11):1678-87. [Content Brief]

Cell Assay ^[2]	Mouse liver cells (BNL CL.2) are maintained in a humidified incubator under 5% CO2 at 37°C in Dulbecco's Modified Eagle's Medium (DMEM). When cells are divided into six-well plates and reach ~90% confluence, sub-confluent cells are washed three times with phosphate buffered saline (PBS) and replaced with serum-free DMEM supplemented with 1% fatty acid-free BSA. Oleic acid (final concentration 500 μM) and GW4064 at various concentrations are added and incubated for 24 h. Cells are then fixed with 4% formaldehyde for Oil Red O staining or harvested for protein and western blot analysis^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]^[3]	Mice^[2] Fifteen-week-old male C57BL/6 mice are fed a high-fat diet with or without additional 0.2% Cholesterol and received twice weekly injections of GW 4064 (50 mg/kg, intra-peritoneal) or carrier solution (DMSO) solution for 6 weeks. Animals are weighed weekly and their body composition is determined using EchoMRI-100^TM from Echo Medical Systems. Rats^[3] Animals. Adult male CRL:CD(SD)IGS rats weighing 300-350 g, are used. Twenty-four hours after laparotomy, groups of rats (n=6) receive intraperitoneal injections once daily for 4 days. Bile duct-ligated (BDL) rats are treated with 5 mL/kg corn oil as vehicle, 30 mg/kg GW4064 in corn oil, or 15 mg/kg TUDCA in corn oil. Sham-operated animals received 5 mL/kg corn oil vehicle. Four hours after the final dose, serum and livers are collected for analysis. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Akwabi-Ameyaw A, 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. [Content Brief] [2]. Ma Y, et al. Synthetic FXR agonist GW4064 prevents diet-induced hepatic steatosis and resistance. Pharm Res. 2013 May;30(5):1447-57. [Content Brief] [3]. Liu Y, et al. Hepatoprotection by the farnesoid X receptor agonist GW4064 in rat models of intra- and extrahepatic cholestasis. J Clin Invest. 2003 Dec;112(11):1678-87. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / DMF	1 mM	1.8422 mL	9.2108 mL	18.4216 mL	46.0541 mL
	5 mM	0.3684 mL	1.8422 mL	3.6843 mL	9.2108 mL
	10 mM	0.1842 mL	0.9211 mL	1.8422 mL	4.6054 mL
	15 mM	0.1228 mL	0.6141 mL	1.2281 mL	3.0703 mL
	20 mM	0.0921 mL	0.4605 mL	0.9211 mL	2.3027 mL
	25 mM	0.0737 mL	0.3684 mL	0.7369 mL	1.8422 mL
	30 mM	0.0614 mL	0.3070 mL	0.6141 mL	1.5351 mL
	40 mM	0.0461 mL	0.2303 mL	0.4605 mL	1.1514 mL
	50 mM	0.0368 mL	0.1842 mL	0.3684 mL	0.9211 mL
	60 mM	0.0307 mL	0.1535 mL	0.3070 mL	0.7676 mL
	80 mM	0.0230 mL	0.1151 mL	0.2303 mL	0.5757 mL
	100 mM	0.0184 mL	0.0921 mL	0.1842 mL	0.4605 mL

GW 4064 Related Classifications

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:

GW 4064278779-30-9GW4064GW-4064FXRAutophagyNR1H4Inhibitorinhibitorinhibit

Please select a local distributor ナミキ商事株式会社コスモ・バイオ株式会社重松貿易株式会社
Product Name			Requested Quantity *
Applicant Name *			Salutation
Email Address *			Phone Number *
Department			Organization Name *
City			State
Country or Region *
Remarks

Product Name			Lot #
Applicant Name *			Email Address *
Phone Number			Department *
Organization Name *			Country or Region *
Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

GW 4064

Customer Review

Other Forms of GW 4064:

GW 4064 Related Antibodies

56 Publications Citing Use of MCE GW 4064

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

GW 4064 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

GW 4064 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report