LXR-623

SKU: orb1307456

Description

LXR-623 (WAY-252623) is a potent and selective synthetic Liver X Receptor (LXR) modulator with oral bioavailability. It is utilized in research to investigate LXR pathways in lipid metabolism and inflammation, with applications in both in vitro assays and in vivo animal studies.

Research Area

Metabolism Research

Key Properties

• CAS Number: 875787-07-8
• MW: 422.78
• Purity: 99.21%
• Formula: C₂₁H₁₂ClF₅N₂
• SMILES: Fc1ccc(cc1)-c1n(Cc2ccc(F)cc2Cl)nc2c(cccc12)C(F)(F)F
• Target: Liver X Receptor
• Solubility: Ethanol:42.3 mg/mL (100.05 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.73 mM);DMSO:42.3 mg/mL (100.05 mM)

Bioactivity

• Target IC50:
  LXRβ:24 nM|LXRα:179 nM
• In Vivo:
  LXR-623 is absorbed rapidly with peak concentrations (Cmax) achieved at approximately 2 hours. The Cmax and area under the concentration-time curve increases in a dose-proportional manner. The mean terminal disposition half-life is between 41 and 43 hours independently of dose. In a low-density lipoprotein (LDL) receptor, (LDLr) knockout mouse model of atherosclerosis, LXR-623 administered orally upregulates intestinal ABCG5 and ABCG8 and reduces atheroma burden without altering serum or hepatic cholesterol and trig-lycerides. LXR-623 shows brain penetration and causes tumor regression in a GBM(glioblastomas) mouse model, reducing cholesterol and inducing cell death.
• In Vitro:
  LXR-623 suppresses LDLR expression, increases expression of the ABCA1 efflux transporter, and induces substantial cell death in all of the GBM samples tested. The brain metastatic breast cancer cell line MDA-MB-361, which harbors ERBB2 amplification, is also highly sensitive to LXR-623- dependent cell death in a concentration-dependent manner. LXR-623 inhibits LDL uptake and induces cholesterol efflux in GBM cells, resulting in a significant reduction in cellular cholesterol content. Normal brain cell insensitivity to LXR-623 may be due to reliance on endogenous synthesis of cholesterol and intact negative feedback through synthesis of endogenous oxysterols.
• Cell Research:
  The purified PBMC are resuspended in culture medium (RPMI + 10% fetal calf serum + 1% penicillin/streptomycin with 1% L-glutamine), transferred to 6-well (9.5 cm2 each) tissue culture dishes at approximately 5 × 106 cells per well, and 2 μM LXR-623 or vehicle (DMSO) are added. After 18 hours of culture, RNA isolation and qPCR analysis for LXRα, LXRβ, ABCA1, ABCG1, and PLTP is performed.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, Liver X receptor, Liver X Receptor, LiverXReceptor, inhibit, LXRα, LXRβ, LXR, LXR 623, LXR623, LXR-623, WAY252623, WAY-252623, WAY 252623

Compound Identifiers

PubChem CID

16734800