GW 4064
Synonym(s):3-(2,6-Dichlorophenyl)-4-(3’-carboxy-2-chlorostilben-4-yl)oxymethyl-5-isopropylisoxazole
- CAS NO.:278779-30-9
- Empirical Formula: C28H22Cl3NO4
- Molecular Weight: 542.84
- MDL number: MFCD09971006
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-09-08 17:00:39
What is GW 4064?
The Uses of GW 4064
A novel nonsteroidal FXR nuclear receptor agonist
The Uses of GW 4064
A novel nonsteroidal FXR nuclear receptor agonist.
The Uses of GW 4064
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
What are the applications of Application
GW 4064 is a novel nonsteroidal FXR nuclear receptor activator
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.
Properties of GW 4064
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 |
Safety information for GW 4064
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral H319:Serious eye damage/eye irritation H413:Hazardous to the aquatic environment, long-term hazard |
Precautionary Statement Codes |
P273:Avoid release to the environment. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for GW 4064
New Products
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