Catalog Number: 2474
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.
Technical Data
  • M.Wt:
    618.51
  • Formula:
    C33H31NO3ClF3.HCl
  • Solubility:
    Soluble to 100 mM in DMSO and to 20 mM in ethanol
  • Purity:
    >98%
  • Storage:
    Desiccate at RT
  • CAS No:
    405911-17-3
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.
Additional Information
Licensing Caveats:
Sold for research purposes under agreement from GlaxoSmithKline
Background References
  1. Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines.
    Collins et al.
    J.Med.Chem., 2002;45:1963
  2. GW3965, a synthetic liver X receptor (LXR) agonist, reduces angiotensin II-mediated pressor responses in Sprague-Dawley rats.
    Leik et al.
    Br.J.Pharmacol., 2007;151:450
  3. Synthetic LXR ligand inhibits the development of atherosclerosis in mice
    Joseph et al.
    Proc.Natl.Acad.Sci.USA, 2002;99:7604
Citations:

The citations listed below are publications that use Tocris products. Selected citations for GW 3965 hydrochloride include:

8 Citations: Showing 1 - 8
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  1. Liver X receptor activation promotes differentiation of regulatory T cells.
    Authors: Herold
    PLoS One 2017;12(9):e0184985
  2. Polarization of M2 macrophages requires Lamtor1 that integrates cytokine and amino-acid signals
    Authors: Kimura Et al.
    Nature Communications 2016;7:13130
  3. Retinoid X receptors orchestrate osteoclast differentiation and postnatal bone remodeling.
    Authors: Menéndez-Gutiérrez Et al.
    PLoS One 2015;125:809
  4. Antiproliferative effects and mechanisms of liver X receptor ligands in pancreatic ductal adenocarcinoma cells.
    Authors: Candelaria Et al.
    Drug Metab Dispos 2014;9:e106289
  5. Regulation of human cytosolic sulfotransferases 1C2 and 1C3 by nuclear signaling pathways in LS180 colorectal adenocarcinoma cells.
    Authors: Rondini Et al.
    J Allergy Clin Immunol 2014;42:361
  6. Human receptor activation by aroclor 1260, a polychlorinated biphenyl mixture.
    Authors: Wahlang Et al.
    Toxicol Sci 2014;140:283
  7. Central diabetes insipidus associated with impaired renal aquaporin-1 expression in mice lacking liver X receptor β.
    Authors: Gabbi Et al.
    Proc Natl Acad Sci U S A 2012;109:3030
  8. Murine atopic dermatitis responds to peroxisome proliferator-activated receptors α and β/δ (but not γ) and liver X receptor activators.
    Authors: Hatano Et al.
    Bioorg Med Chem Lett 2010;125:160

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