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GW-4064

Chemical Structure : GW-4064

CAS No.: 278779-30-9

GW-4064 (GW 4064;GW4064)

Catalog No.: PC-45825Not For Human Use, Lab Use Only.

GW-4064 (GW4064) is a potent and selective FXR agonist with EC50 of 15 nM in cell-free assay, >200-fold more potent than CDCA.

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Biological Activity

GW-4064 (GW4064) is a potent and selective FXR agonist with EC50 of 15 nM in cell-free assay, >200-fold more potent than CDCA.
GW-4064 has an EC50 of 80 and 90 nM, respectively, in CV-1 cells transfected with mouse and human FXR expression vectors.
GW-4064 significantly reducess serum alanine aminotransferase, aspartate aminotransferase, and lactate dehydrogenase, as well as other markers of liver damage in rat models of cholestasis.

Physicochemical Properties

M.Wt 542.8376
Formula C28H22Cl3NO4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

1. Maloney PR, et al. J Med Chem. 2000 Aug 10;43(16):2971-4.

2. Liu Y, et al. J Clin Invest. 2003 Dec;112(11):1678-87.

3. Kast HR, et al. J Biol Chem. 2002 Jan 25;277(4):2908-15.

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