GW3965 HCl

SKU: orb1300880

Description

GW3965 HCl is a potent and selective agonist of liver X receptors α and β (LXRα/β), exhibiting EC50 values of 190 nM and 30 nM, respectively. This compound is widely used in research to investigate LXR pathways in lipid metabolism, inflammation, and atherosclerosis, employing both in vitro and in vivo experimental models.

Research Area

Neuroscience

Key Properties

• CAS Number: 405911-17-3
• MW: 618.5
• Purity: >98%
• Formula: C₃₃H₃₁ClF₃NO₃ • HCl
• SMILES: c1ccc(cc1)C(CN(CCCOc1cccc(c1)CC(=O)O)Cc1c(c(ccc1)C(F)(F)F)Cl)c1ccccc1.Cl
• Target: Transcription factor
• Solubility: Soluble in DMSO (up to 48 mg/ml)

Bioactivity

• Target IC50:
  LXRα (human):190 nM (EC50)|LXRβ (human):30 nM (EC50)
• 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 (10 mg/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.
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• In Vitro:
  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.
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• Cell Research:
  Cells are seeded in 96 wells and are treated after 24 hours with different drugs indicated in each experiment in medium containing 1% FBS or lipoprotein deficient serum. Relative proliferation is determined using Cell Proliferation Assay Kit. Cells are incubated 1.5 hrs after adding tetrazolium salt WST-1 [2-(4-iodophenyl)-3- (4-nitrophenyl)-5-(2, 4-disulfo-phenyl)-2H-tetrazolium, monosodium salt] at 5% CO2, 37oC and the absorbance of the treated and untreated cells are measured using a microplate reader at 420 to 480 nm. Cells seeded in 12 well plates are counted using a hemocytometer, and dead cells are assessed using trypan blue exclusion assays.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

hLXRα, hLXRβ, GW 3965, GW 3965 Hydrochloride, GW3965, GW-3965, GW3965 HCl, GW3965 Hydrochloride, GW3965 hydrochloride, GW-3965 hydrochloride, GW-3965 Hydrochloride, inhibit, Inhibitor, LXR, LXRα/SRC1 LiSA, LiverXReceptor, Liver X Receptor, Liver X receptor

Compound Identifiers

PubChem CID

16078973