GW 4064

Product Description

GW 4064 is a potent and selective, non-steroidal farnesoid X receptor (FXR) agonist (EC₅₀ = 15 nM). GW 4064 displays no activity at other nuclear receptors at concentrations up to 1 μM. Improves hyperglycaemia and hyperlipidemia in diabetic db/db mice. Shown to suppress autophagy in nutrient-deprived mouse hepatocytes. GW 4064 protects against lipopolysaccharide (LPS)-induced liver inflammation and apoptosis in mice. GW 4064 reduces Leptin signaling pathway activation in breast cancer cells and inhibits tumor growth in mouse xenografts.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline

Solubility

Preparing Stock Solutions for GW 4064

The following data is based on the product molecular weight 542.84

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.84 mL	9.21 mL	18.42 mL
5 mM	0.37 mL	1.84 mL	3.68 mL
10 mM	0.18 mL	0.92 mL	1.84 mL
50 mM	0.04 mL	0.18 mL	0.37 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Giordano Activated FXR inhibits leptin signaling and counteracts tumor-promoting activities of cancer-associated fibroblasts in breast malignancy. Sci.Rep. 2016 PMID: 26899873
• Liu GW4064 attenuates lipopolysaccharide induced hepatic inflammation and apoptosis through inhibition of the Toll like receptor 4 mediated p38 mitogen activated protein kinase signalling pathway in mice. Int.J.Mol.Med. 2018 PMID: 29328388
• Lee Nutrient-sensing nuclear receptors coordinate autophagy. Nature 2014 PMID: 25383539
• Zhang Activation of the nuclear receptor FXR improves hyperglycemia and hyperlipidemia in diabetic mice. Proc.Natl.Acad.Sci.USA
• Cariou The farnesoid X receptor modulates adiposity and peripheral Ins sensitivity in mice. J.Biol.Chem. 2006 PMID: 16446356
• Maloney Identification of a chemical tool for the orphan nuclear receptor FXR. J.Med.Chem. 2000 PMID: 10956205