G5172
GW4064
≥97% (HPLC), farnesoid X receptor agonist, powder
Synonym(s):
3-(2,6-Dichlorophenyl)-4-(3’-carboxy-2-chlorostilben-4-yl)oxymethyl-5-isopropylisoxazole
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About This Item
Empirical Formula (Hill Notation):
C28H22Cl3NO4
CAS Number:
Molecular Weight:
542.84
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.32
MDL number:
Product Name
GW4064, ≥97% (HPLC)
Quality Level
assay
≥97% (HPLC)
form
powder
storage condition
desiccated
color
white
solubility
DMSO: 10 mg/mL, clear
storage temp.
2-8°C
SMILES string
CC(C)c1onc(c1COc2ccc(\C=C\c3cccc(c3)C(O)=O)c(Cl)c2)-c4c(Cl)cccc4Cl
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+
InChI key
BYTNEISLBIENSA-MDZDMXLPSA-N
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.
Application
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
Biochem/physiol Actions
GW4064 is a FXR agonist.
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.
Features and Benefits
This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral - Aquatic Chronic 4 - Eye Irrit. 2
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
dust mask type N95 (US), Eyeshields, Gloves
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Esther M Verhaag et al.
PloS one, 11(3), e0149782-e0149782 (2016-03-08)
Cholestasis is characterized by accumulation of bile acids and inflammation, causing hepatocellular damage. Still, liver damage markers are highest in acute cholestasis and drop when this condition becomes chronic, indicating that hepatocytes adapt towards the hostile environment. This may be
Sarah Farr et al.
American journal of physiology. Gastrointestinal and liver physiology, 318(4), G682-G693 (2020-02-01)
Postprandial dyslipidemia is a common feature of insulin-resistant states and contributes to increased cardiovascular disease risk. Recently, bile acids have been recognized beyond their emulsification properties as important signaling molecules that promote energy expenditure, improve insulin sensitivity, and lower fasting
Farnesoid X receptor agonist GW4064 ameliorates lipopolysaccharide-induced ileocolitis through TLR4/MyD88 pathway related mitochondrial dysfunction in mice
Liu HM, et al.
Biochemical and Biophysical Research Communications, 490(3), 841-848 (2017)
Global Trade Item Number
| SKU | GTIN |
|---|---|
| G5172-5MG | 04061833633472 |
| G5172-25MG | 04061831238945 |