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[CAS NO. 278779-30-9] GW4064

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Catalog:	HY-50108
Brand:	MCE
CAS:	278779-30-9

Overview

MDL	MFCD09971006
Molecular Weight	542.84
Molecular Formula	C28H22Cl3NO4
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

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

23 Publications Citing Use of MCE

[1]Research (Wash D C). 2022 Nov 2;2022:9784081.
[2]Dev Cell. 2019 Feb 25;48(4):460-474.e9.
[3]J Am Soc Nephrol. 2019 Jun;30(6):962-978.
[4]Theranostics. 2022 Aug 15;12(14):6130-6142.
[5]Cell Rep. 2021 Jul 20;36(3):109398.
[6]Acta Pharm Sin B. 2019 May;9(3):526-536.
[7]Sci Total Environ. 2023 Apr 15.
[8]JCI Insight. 2020 Dec 8;141640.
[9]EBioMedicine. 2018 Nov;37:322-333.
[10]FASEB J. 2022 Apr;36(4):e22243.
[11]FASEB J. 2019 Feb;33(2):2472-2483.
[12]Int J Mol Sci. 2018 Jun 28;19(7). pii: E1898.
[13]iScience. 19 August 2021, 103003.
[14]Commun Biol. 2022 Jul 28;5(1):750.
[15]J Transl Med. 2019 Dec 13;17(1):418.
[16]Am J Transl Res. 2021 Aug 15;13(8):9296-9305.
[17]Aquaculture. 2021, 736248.
[18]Nutr Metab. 2022 Aug 23;19(1):57.
[19]FEBS Lett. 2017 Sep;591(18):2836-2847.
[20]Phytochemistry. 2022.
[21]J Pharm Anal. 2020 Jan.
[22]Biotechnol Lett. 2020 Aug;42(8):1327-1336.
[23]Patent. US20200368199A1.

Summary

GW 4064 is a potent FXR agonist with an EC ₅₀ of 65 nM.

IC50 & Target

EC50: 65 nM (FXR) ^[1]

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] .

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] .

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

Appearance

Solid

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)

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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

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
2.

Add each solvent one by one: 10% DMF >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.61 mM); Clear solution
3.

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
4.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (3.83 mM); Clear solution

* All of the co-solvents are available by MCE.

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

Synonyms

Benzoic acid, 3-[2-[2-chloro-4-[[3-(2,6-dichlorophenyl)-5-(1-methylethyl)-4-isoxazolyl]methoxy]phenyl]ethenyl]-

3-[2-[2-Chloro-4-[[3-(2,6-dichlorophenyl)-5-(1-methylethyl)-4-isoxazolyl]methoxy]phenyl]ethenyl]benzoic acid

GW 4064

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