GW 3965 hydrochloride

Cat. No. 2474

GW 3965 hydrochloride C33H31NO3ClF3.HCl [405911-17-3]

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Chemical Name: 3-[3-[[[2-Chloro-3-(trifluoromethyl)phenyl]methyl](2,2-diphenylethyl)amino]propoxy]benzeneacetic acid hydrochloride

Biological Activity

Selective, orally active non-steroidal agonist for the liver X receptor (LXR). In cell-based reporter gene assays, acts as a full agonist of hLXRα and hLXRβ (EC50 values are 190 and 30 nM respectively). Reduces angiotensin II-mediated increases in blood pressure; up-regulates ABCA1 gene expression and raises circulating HDL levels. Displays potent antiatherogenic activity in mouse models of atherosclerosis.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline

Technical Data

Soluble to 100 mM in DMSO and to 20 mM in ethanol
>98 %
Desiccate at RT

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

Leik et al (2007) GW3965, a synthetic liver X receptor (LXR) agonist, reduces angiotensin II-mediated pressor responses in Sprague-Dawley rats. Br.J.Pharmacol. 151 450. PMID: 17420776.

Collins et al (2002) Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines. J.Med.Chem. 45 1963. PMID: 11985463.

Joseph et al (2002) Synthetic LXR ligand inhibits the development of atherosclerosis in mice Proc.Natl.Acad.Sci.USA 99 7604.

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Citations are publications that use Tocris products. Selected citations for GW 3965 hydrochloride include:

Menéndez-Gutiérrez et al (2015) Retinoid X receptors orchestrate osteoclast differentiation and postnatal bone remodeling. PLoS One 125 809. PMID: 25574839.

Candelaria et al (2014) Antiproliferative effects and mechanisms of liver X receptor ligands in pancreatic ductal adenocarcinoma cells. Drug Metab Dispos 9 e106289. PMID: 25184494.

Rondini et al (2014) Regulation of human cytosolic sulfotransferases 1C2 and 1C3 by nuclear signaling pathways in LS180 colorectal adenocarcinoma cells. J Allergy Clin Immunol 42 361. PMID: 24335393.

Wahlang et al (2014) Human receptor activation by aroclor 1260, a polychlorinated biphenyl mixture. Toxicol Sci 140 283. PMID: 24812009.

Gabbi et al (2012) Central diabetes insipidus associated with impaired renal aquaporin-1 expression in mice lacking liver X receptor β. Proc Natl Acad Sci U S A 109 3030. PMID: 22323586.

Hatano et al (2010) Murine atopic dermatitis responds to peroxisome proliferator-activated receptors α and β/δ (but not γ) and liver X receptor activators. Bioorg Med Chem Lett 125 160. PMID: 19818482.

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Keywords: GW 3965 hydrochloride, supplier, non-steroidal, liver, X, receptor, LXR, agonists, FXR, Receptors, Farnesoid, LXR-like, GW3965, hydrochloride, GlaxoSmithKline, GSK, Tocris Bioscience, LXR-like Receptor Agonist products

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