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Submit ReviewGW 3965 hydrochloride
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)
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 |
| InChI Key | NMPUWJFHNOUNQU-UHFFFAOYSA-N |
| 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 | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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
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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Keywords: GW 3965 hydrochloride, GW 3965 hydrochloride supplier, non-steroidal, liver, X, receptor, LXR, agonists, FXR, Receptors, Farnesoid, LXR-like, GW3965, hydrochloride, GlaxoSmithKline, GSK, 2474, Tocris Bioscience
10 Citations for GW 3965 hydrochloride
Citations are publications that use Tocris products. Selected citations for GW 3965 hydrochloride include:
Kimura et al (2016) Polarization of M2 macrophages requires Lamtor1 that integrates cytokine and amino-acid signals Nature Communications 7 13130 PMID: 27731330
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
Menéndez-Gutiérrez et al (2015) Retinoid X receptors orchestrate osteoclast differentiation and postnatal bone remodeling. PLoS One 125 809 PMID: 25574839
Wahlang et al (2014) Human receptor activation by aroclor 1260, a polychlorinated biphenyl mixture. Toxicol Sci 140 283 PMID: 24812009
Gibson et al (2018) The impact of 27-hydroxycholesterol on endometrial cancer proliferation. Endocr Relat Cancer 25 381 PMID: 29371332
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
Herold (2017) Liver X receptor activation promotes differentiation of regulatory T cells. PLoS One 12 e0184985 PMID: 28926619
Dong et al (2019) 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. Int J Mol Med 43 1927 PMID: 30896855
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
Do you know of a great paper that uses GW 3965 hydrochloride from Tocris? Please let us know.
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