Toggle Nav
Close
  • Menu
  • Setting

GW3965 HCl

Catalog No.
A8444
LXR agonist, selective and orally active
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$100.00
In stock
5mg
$69.00
In stock
10mg
$105.00
In stock
50mg
$399.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

GW3965 HCl is a selective, orally active non-steroidal agonist for the liver X receptor (LXR) [1].
Nuclear receptors LXRα  and LXRβ have an important role in control of cholesterol and fatty acid metabolism in multiple cell types. Activation of these receptors promotes bile acid synthesis in liver, inhibits intestinal cholesterol absorption and stimulates cholesterol efflux in macrophages, which will then reduce atherosclerotic risk [2].
In a cell-free ligand-sensing assay, GW3965 recruits the steroid receptor coactivator 1 to human LXRR with an EC50 of 125 nM. In cell-based reporter gene assays, GW3965 plays as a full agonist on hLXRα and hLXRβ with EC50 of 190 and 30 nM, respectively [1].
Treatment C57BL/6 mice with 10 mg/kg GW3965 HCl orally, GW3965 HCl increased the plasma concentrations of HDL cholesterol by 30% and enhanced the expression of the reverse cholesterol transporter ABCA1 in the small intestine and peripheral macrophages [1]. In male Sprague–Dawley rats, GW3965 decreased Ang II-mediated vasopressor responses and reduced ATR gene expression, which suggested GW3965 can affect vascular reactivity [3].
References:
[1]. Collins JL, Fivush AM, Watson MA, et al. Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines. J Med Chem, 2002, 45(10): 1963-1966.
[2]. Joseph SB, McKilligin E, Pei L, et al. Synthetic LXR ligand inhibits the development of atherosclerosis in mice. Proc Natl Acad Sci U S A, 2002, 99(11): 7604-7609.
[3]. Leik CE, Carson NL, Hennan JK, et al. GW3965, a synthetic liver X receptor (LXR) agonist, reduces angiotensin II-mediated pressor responses in Sprague-Dawley rats. Br J Pharmacol, 2007, 151(4): 450-456.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt618.51
Cas No.405911-17-3
FormulaC33H31ClF3NO3·HCl
Solubility≥30.55mg/mL in DMSO
Chemical Name2-[3-[3-[[2-chloro-3-(trifluoromethyl)phenyl]methyl-(2,2-diphenylethyl)amino]propoxy]phenyl]acetic acid;hydrochloride
SDFDownload SDF
Canonical SMILESC1=CC=C(C=C1)C(CN(CCCOC2=CC=CC(=C2)CC(=O)O)CC3=C(C(=CC=C3)C(F)(F)F)Cl)C4=CC=CC=C4.Cl
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Quality Control