GW 3965 hydrochloride

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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% (HPLC)
Citations (10)

Biological Activity for GW 3965 hydrochloride

GW 3965 hydrochloride is a 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

Compound Libraries for GW 3965 hydrochloride

GW 3965 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for GW 3965 hydrochloride

M. Wt 618.51
Formula C33H31NO3ClF3.HCl
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 405911-17-3
PubChem ID 16078973
Smiles Cl.OC(=O)CC1=CC=CC(OCCCN(CC(C2=CC=CC=C2)C2=CC=CC=C2)CC2=C(Cl)C(=CC=C2)C(F)(F)F)=C1

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.

Solubility Data for GW 3965 hydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 61.85 100
ethanol 12.37 20

Preparing Stock Solutions for GW 3965 hydrochloride

The following data is based on the product molecular weight 618.51. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.62 mL 8.08 mL 16.17 mL
5 mM 0.32 mL 1.62 mL 3.23 mL
10 mM 0.16 mL 0.81 mL 1.62 mL
50 mM 0.03 mL 0.16 mL 0.32 mL

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Product Datasheets for GW 3965 hydrochloride

Certificate of Analysis / Product Datasheet
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References for GW 3965 hydrochloride

References are publications that support the biological activity of the product.

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

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

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

If you know of a relevant reference for GW 3965 hydrochloride, please let us know.

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10 Citations for GW 3965 hydrochloride

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

Gibson et al (2018) The impact of 27-hydroxycholesterol on endometrial cancer proliferation. Endocr Relat Cancer 25 381 PMID: 29371332

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

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

Do you know of a great paper that uses GW 3965 hydrochloride from Tocris? Please let us know.

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