GW 3965 hydrochloride

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GW 3965 hydrochloride | CAS No. 405911-17-3 | LXR-like Receptor Agonists
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Description: Orally active liver X receptor (LXR) agonist

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

Purity: ≥98%

Product Details
Citations (10)
Reviews

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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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

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Citations for GW 3965 hydrochloride

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

10 Citations: Showing 1 - 10

  1. Activation of FXR by obeticholic acid induces hepatic gene expression of SR-BI through a novel mechanism of transcriptional synergy with the nuclear receptor LXR.
    Authors: Dong Et al.
    Int J Mol Med  2019;43:1927
  2. The impact of 27-hydroxycholesterol on endometrial cancer proliferation.
    Authors: Gibson Et al.
    Endocr Relat Cancer  2018;25:381
  3. Liver X receptor activation promotes differentiation of regulatory T cells.
    Authors: Herold
    PLoS One  2017;12(9):e0184985
  4. Polarization of M2 macrophages requires Lamtor1 that integrates cytokine and amino-acid signals
    Authors: Kimura Et al.
    Nature Communications  2016;7:13130
  5. Retinoid X receptors orchestrate osteoclast differentiation and postnatal bone remodeling.
    Authors: Menéndez-Gutiérrez Et al.
    PLoS One  2015;125:809
  6. Antiproliferative effects and mechanisms of liver X receptor ligands in pancreatic ductal adenocarcinoma cells.
    Authors: Candelaria Et al.
    Drug Metab Dispos  2014;9:e106289
  7. 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
  8. Human receptor activation by aroclor 1260, a polychlorinated biphenyl mixture.
    Authors: Wahlang Et al.
    Toxicol Sci  2014;140:283
  9. 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
  10. 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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