GW 4064

• CAT Number: I002951
• CAS Number: 278779-30-9
• Molecular Formula: C28H22Cl3NO4
• Molecular Weight: 542.8
• Purity: ≥95%
• Target: FXR
• Solubility: 10 mM in DMSO
• Storage: 2-8°C
• IC50: 15 nM (EC50)
• IUPAC Name: 3-[(E)-2-[2-chloro-4-[[3-(2,6-dichlorophenyl)-5-propan-2-yl-1,2-oxazol-4-yl]methoxy]phenyl]ethenyl]benzoic acid
• InChI: InChI=1S/C28H22Cl3NO4/c1-16(2)27-21(26(32-36-27)25-22(29)7-4-8-23(25)30)15-35-20-12-11-18(24(31)14-20)10-9-17-5-3-6-19(13-17)28(33)34/h3-14,16H,15H2,1-2H3,(H,33,34)/b10-9+
• InChIKey: BYTNEISLBIENSA-MDZDMXLPSA-N
• SMILES: CC(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

GW4064（Cat No.:I002951） is a potent agonist of the farnesoid X receptor (FXR), with an EC50 of 65 nM in CV1 cell line. It exhibits no significant activity on other nuclear receptors at concentrations up to 1 μM. In addition to its role as an FXR agonist, GW4064 has been found to stimulate autophagy in MCF-7 cells. This finding suggests a potential dual mechanism of action for GW4064, highlighting its relevance in both FXR modulation and autophagy regulation.

Reference

1:FXR agonist activity of conformationally constrained analogs of GW 4064. Akwabi-Ameyaw A, Bass JY, Caldwell RD, Caravella JA, Chen L, Creech KL, Deaton DN, Madauss KP, Marr HB, McFadyen RB, Miller AB, Navas F 3rd, Parks DJ, Spearing PK, Todd D, Williams SP, Bruce Wisely G.Bioorg Med Chem Lett. 2009 Aug 15;19(16):4733-9. doi: 10.1016/j.bmcl.2009.06.062. Epub 2009 Jun 21. PMID: 19586769 2:Conformationally constrained farnesoid X receptor (FXR) agonists: Naphthoic acid-based analogs of GW 4064. Akwabi-Ameyaw A, Bass JY, Caldwell RD, Caravella JA, Chen L, Creech KL, Deaton DN, Jones SA, Kaldor I, Liu Y, Madauss KP, Marr HB, McFadyen RB, Miller AB, Navas F III, Parks DJ, Spearing PK, Todd D, Williams SP, Wisely GB.Bioorg Med Chem Lett. 2008 Aug 1;18(15):4339-43. doi: 10.1016/j.bmcl.2008.06.073. Epub 2008 Jun 28. PMID: 18621523