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GW4064

In stock
Catalog No.
B1527
Non-steroidal FXR agonist,potent and selective
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$67.00
In stock
5mg
$50.00
In stock
10mg
$80.00
In stock
50mg
$260.00
In stock

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Email: [email protected]

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GW4064 is an agonist of FXR with EC50 values of 15nM and 90nM, respectively in an isolated receptor activity assay and in cells transfected with human FXR [1].

GW4064 is identified as a highly effective, selective, nonsteroidal agonist of FXR. It shows beneficial effects on cholesterol and TG in various animal species. GW4064 is found to lower serum TG levels in both the KK-Ay and ob/ob mice potently. In KK-Ay mice, a 1-week administration of GW4064 also significantly lowers VLDL secretion. And in the SHP+/+ mice, GW4064 can also lower serum TGs. [2]

Due to some limitations, such as limited solubility, potentially toxic stilbene pharmacophore and UV light instability, GW4064 is not a good candidate of drug. It is now usually used as a tool compound for investigating the physiological functions of FXR [3].

References:
[1] Chiang PC, Thompson DC, Ghosh S, Heitmeier MR. A formulation-enabled preclinical efficacy assessment of a farnesoid X receptor agonist, GW4064, in hamsters and cynomolgus monkeys. J Pharm Sci. 2011 Nov;100(11):4722-33.
[2] Watanabe M, Houten SM, Wang L, Moschetta A, Mangelsdorf DJ, Heyman RA, Moore DD, Auwerx J. Bile acids lower triglyceride levels via a pathway involving FXR, SHP, and SREBP-1c. J Clin Invest. 2004 May;113(10):1408-18.
[3] Li W, Fu J, Cheng F, Zheng M, Zhang J, Liu G, Tang Y. Unbinding pathways of GW4064 from human farnesoid X receptor as revealed by molecular dynamics simulations. J Chem Inf Model. 2012 Nov 26;52(11):3043-52.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt542.85
Cas No.278779-30-9
FormulaC28H22Cl3NO4
Solubility≥24.7mg/mL in DMSO
Chemical Name3-[(E)-2-[2-chloro-4-[[3-(2,6-dichlorophenyl)-5-propan-2-yl-1,2-oxazol-4-yl]methoxy]phenyl]ethenyl]benzoic acid
SDFDownload SDF
Canonical SMILESCC(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
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description GW4064 is a selective non-steroidal agonist of farnesoid X receptor (FXR) with EC50 value of 15 nM.
Targets FXR          
IC50 15 nM (EC50)          

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