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Merck

G5172

GW4064

≥97% (HPLC), farnesoid X receptor agonist, powder

Sinónimos:

3-(2,6-Dichlorophenyl)-4-(3’-carboxy-2-chlorostilben-4-yl)oxymethyl-5-isopropylisoxazole

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Acerca de este artículo

Fórmula empírica (notación de Hill):
C28H22Cl3NO4
Número CAS:
Peso molecular:
542.84
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.32
MDL number:
Assay:
≥97% (HPLC)
Form:
powder
Quality level:
Storage condition:
desiccated
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Nombre del producto

GW4064, ≥97% (HPLC)

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

assay

≥97% (HPLC)

form

powder

storage condition

desiccated

color

white

solubility

DMSO: 10 mg/mL, clear

storage temp.

2-8°C

Quality Level

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.

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.

pictograms

Exclamation mark

signalword

Warning

Hazard Classifications

Acute Tox. 4 Oral - Aquatic Chronic 4 - Eye Irrit. 2

Clase de almacenamiento

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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Synthetic FXR Agonist GW4064 Is a Modulator of Multiple G Protein-Coupled Receptors
Singh N, et al.
Molecular Endocrinology, 28(5), 659-673 (2014)
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Journal of autoimmunity, 90, 64-75 (2018-02-13)
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Qixiao Zhai et al.
Food & function, 10(3), 1455-1464 (2019-02-16)
The management of lead (Pb) exposure and toxicity remains a major public health priority worldwide. In our previous study, the probiotic strain Lactobacillus plantarum CCFM8661 prevented Pb absorption in mice via intestinal sequestration. This follow-up study aimed to evaluate the
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
Jing Yang et al.
Frontiers in pharmacology, 8, 260-260 (2017-05-26)
Triptolide (TP), a diterpenoid isolated from

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