Molecular Weight(MW): 618.51
GW3965 HCl is a potent, selective LXR agonist for hLXRα and hLXRβ with EC50 of 190 and 30 nM in cell-free assays, respectively.
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a. Western blot analysis for EpCAM, PKM2, and CK19 expression in livers from C57BL/6J mice treated with DDC for 1 week in the absence or presence of GW3965 (10 mg/kg; n = 4 per group). *P < 0.05, **P < 0.01. c Western blot analysis of p-STAT3, t-STAT3, and SOCS3 in WB-F344 cells treated with GW3965 (5 μM) or DMSO as control in response to IL-6 (50 ng/ml) treatment for 0, 0.25, 0.5, 0.75, 1, and 2 h.
Arch Toxicol, 2017, 91(1):271-287. GW3965 HCl purchased from Selleck.
The effects of GW3965 on NDV infection. (A) The DF-1 cells were cultured with different concentrations of GW3965. Cell viability was determined by MTT assay at 24 h. (B) Synthetic LXR agonist GW3965 inhibited NDV infection in DF-1 cells. Cells were pretreated with GW3965 (1 μM) for 2 h, then infected with NDV (MOI = 1). GW3965 (1 μM) was continuously present during the infection. The expression level of the viral NP protein was determined by western blot. (C) The titers of the supernatant were determined by TCID50. (D) The viral gRNA in cells was detected by qRT-PCR assay.
Arch Virol, 2016, 161(9):2491-501.. GW3965 HCl purchased from Selleck.
Purity & Quality Control
Choose Selective Liver X Receptor Inhibitors
|Description||GW3965 HCl is a potent, selective LXR agonist for hLXRα and hLXRβ with EC50 of 190 and 30 nM in cell-free assays, respectively.|
GW3965 recruits the steroid receptor coactivator 1 to human LXRα with EC50 of 125 nM in a cell-free ligand-sensing assay.  GW3965 shows a potent antagonistic activity against hLXRα and hLXRβ in cell-based assays with EC50 of 190 nM and 30 nM, respectively. Besides, GW3965 also sows excellent selectivity over other nuclear receptors.  In human islets, GW3965 (1 μM) reduces expression of selected pro-inflammatory cytokines including IL-8, monocyte chemotactic protein-1 and tissue factor. 
|In vivo||In mice, GW3965 at a dose of 10 mg/kg upregulates ABCA1 expression 8-fold and raises circulating levels of HDL by 30% with Cmax of 12.7 μg/mL and t1/2 of 2 hours.  GW3965 (10mg/kg) induces expression of ABCA1 and ABCG1 and shows potent antiatherogenic activity in both LDLR−/− and apoE−/− mice.  In male sprague-dawley rats, GW3965 reduces Ang II-mediated increases in blood pressure and decreases vascular Ang II receptor gene expression.  In Glioblastoma mouse model, GW3965 results in inducible degrader of LDLR-mediated LDLR degradation, increased expression of the ABCA1 cholesterol efflux transporter, and thus potently promotes tumor cell death. |
-  Collins JL, et al. J Med Chem. 2002, 45(10), 1963-1966.
-  Joseph SB, et al. Proc Natl Acad Sci U S A. 2002, 99(11), 7604-7609.
-  Leik CE, et al. Br J Pharmacol. 2007, 151(4), 450-456.
|In vitro||DMSO||16 mg/mL warmed (25.86 mM)|
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Frequently Asked Questions
How to formulate the compound for mouse in vivo experiment?
S2630 GW3965 HCl can be dissolved in 2% DMSO/30% PEG 300/dd H2O at 10 mg/mL as a homogeneous suspension. This vehicle is suitable for oral gavage to mice.