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| GW 4064 Basic information |
| Product Name: | GW 4064 | | Synonyms: | GW 4064;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]-benzoic Acid;GW 4064,3-[2-[2-Chloro-4-[[3-(2,6-dichlorophenyl)-5-(1-methylethyl)-4-isoxazolyl]methoxy]phenyl]ethenyl]benzoicacid;CS-278;GW4064;GW 4064;3-(2,6-Dichlorophenyl)-4-(3'-carboxy-2-chlorostilben-4-yl)oxymethyl-5-isopropylisoxazole;3-[2-[2-Chloro-4-[[3-(2,6-dichlorophenyl)-5-isopropylisoxazol-4-yl]Methoxy]phenyl]vinyl]benzoic acid | | CAS: | 278779-30-9 | | MF: | C28H22Cl3NO4 | | MW: | 542.84 | | EINECS: | | Product Categories: | Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;API | | Mol File: | 278779-30-9.mol |
| GW 4064 Chemical Properties |
| 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 | | pka | 4.13±0.10(Predicted) | | form | powder | | color | white |
| Hazard Codes | Xn | | Risk Statements | 22-36 | | Safety Statements | 26 | | WGK Germany | 3 |
| GW 4064 Usage And Synthesis |
| Uses | A novel nonsteroidal FXR nuclear receptor agonist | | Uses | A novel nonsteroidal FXR nuclear receptor agonist. | | Uses | GW4064 has been used:- to investigate its ability to protect the livers of mice from lipopolysaccharide (LPS)-induced inflammation and apoptosis
- to examine its capability to inhibit mucosal injury in ileum caused by lipopolysaccharide (LPS)
- to treat ileal explants
| | 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. | | 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. |
| GW 4064 Preparation Products And Raw materials |
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