GW 4064 Struktur

GW 4064

Bezeichnung:GW 4064

CAS-Nr278779-30-9

Englisch Name:GW 4064

CBNumberCB8799852

SummenformelC28H22Cl3NO4

Molgewicht542.84

MOL-Datei278779-30-9.mol

GW 4064 physikalisch-chemischer Eigenschaften

Schmelzpunkt	>175°C (dec.)
Siedepunkt	702.1±60.0 °C(Predicted)
Dichte	1.367±0.06 g/cm3(Predicted)
storage temp.	2-8°C
Löslichkeit	DMSO: soluble10mg/mL, clear
pka	4.13±0.10(Predicted)
Aggregatzustand	powder
Farbe	white

Sicherheit

Kennzeichnung gefährlicher	Xn
R-Sätze:	22-36
S-Sätze:	26
WGK Germany	3

Gefahreninformationscode (GHS)

GW 4064 Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R22:Gesundheitsschädlich beim Verschlucken.
R36:Reizt die Augen.
S-Sätze Betriebsanweisung:
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
Verwenden
A novel nonsteroidal FXR nuclear receptor agonist.
Verwenden
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
Definition
ChEBI: GW 4064 is a stilbenoid.
Allgemeine Beschreibung
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.
Biologische Aktivität
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.
Lager
Store at +4°C
Einzelnachweise
[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 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

278779-30-9, GW 4064 Verwandte Suche:

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