| Identification | Back Directory | [Name]
GW 4064 | [CAS]
278779-30-9 | [Synonyms]
CS-278
GW 4064
GW4064;GW 4064
3-(2,6-Dichlorophenyl)-4-(3'-carboxy-2-chlorostilben-4-yl)oxymethyl-5-isopropylisoxazole
3-[2-Chloro-4-[[3-(2,6-dichlorophenyl)-5-isopropyl-4-isoxazolyl]methoxy]styryl]benzoic Acid
3-[2-[2-Chloro-4-[3-(2,6-dichlorophenyl)-5-isopropyl-isoxazol-4-ylMethoxy]phenyl]vinyl]benzoic
GW-4064,3-[2-[2-Chloro-4-[3-(2,6-dichlorophenyl)-5-isopropylisoxazol-4-ylMethoxy]phenyl]vinyl]benzoi
3-[2-[2-Chloro-4-[[3-(2,6-dichlorophenyl)-5-isopropylisoxazol-4-yl]Methoxy]phenyl]vinyl]benzoic acid
3-[2-[2-Chloro-4-[[3-(2,6-Dichlorophenyl)-5-(1-methylethyl)-4-isoxazolyl]methoxy]phenyl]ethenyl]-benzoic Acid
Benzoic acid, 3-[2-[2-chloro-4-[[3-(2,6-dichlorophenyl)-5-(1-Methylethyl)-4-isoxazolyl]Methoxy]phenyl]ethenyl]-
GW 4064,3-[2-[2-Chloro-4-[[3-(2,6-dichlorophenyl)-5-(1-methylethyl)-4-isoxazolyl]methoxy]phenyl]ethenyl]benzoicacid
Benzoic acid, 3-[2-[2-chloro-4-[[3-(2,6-dichlorophenyl)-5-(1-methylethyl)-4-isoxazolyl]methoxy]phenyl]ethenyl]-GW 4064
3-(2,6-Dichlorophenyl)-4-(3'-carboxy-2-chlorostilben-4-yl)oxymethyl-5-isopropylisoxazole GW 4064 | [Molecular Formula]
C28H22Cl3NO4 | [MDL Number]
MFCD08704413 | [MOL File]
278779-30-9.mol | [Molecular Weight]
542.84 |
| Chemical Properties | Back Directory | [Melting point ]
>175°C (dec.) | [Boiling point ]
702.1±60.0 °C(Predicted) | [density ]
1.367±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: soluble10mg/mL, clear | [form ]
powder | [pka]
4.13±0.10(Predicted) | [color ]
white | [InChIKey]
BYTNEISLBIENSA-UHFFFAOYSA-N | [SMILES]
C(O)(=O)C1=CC=CC(C=CC2=CC=C(OCC3=C(C(C)C)ON=C3C3=C(Cl)C=CC=C3Cl)C=C2Cl)=C1 |
| Hazard Information | Back Directory | [Uses]
A novel nonsteroidal FXR nuclear receptor agonist | [Definition]
ChEBI: GW 4064 is a stilbenoid. | [General Description]
GW4064 is a synthetic isoxazole, which is used to decipher the cellular and physiological functions of farnesoid X receptor (FXR). It is an estrogen receptor-related receptors (ERRs) agonist. | [Biological Activity]
Selective, non-steroidal farnesoid X receptor (FXR) agonist (EC 50 = 15 nM). Displays no activity at other nuclear receptors at concentrations up to 1 μ M. Improves hyperglycaemia and hyperlipidaemia in diabetic db/db mice. | [Biochem/physiol Actions]
GW4064 is a FXR agonist. GW4064 is a potent (EC50 = 15 nM), non-steroidal agonist of the orphan nuclear receptor FXR. It shows no activity on other nuclear receptors including RAR up to 1 mM. This is an important tool for the study of the involvment of FXR in a variety of biological activities. | [storage]
Store at +4°C | [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. |
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