Home Metabolism Liver X Receptor agonist LXR-623 For research use only.

LXR-623

Synonyms: WAY-252623

LXR-623 is a novel liver X-receptor(LXR) agonist with IC50 values of 179 nM and 24 nM for LXR-α and LXR-β, respectively. It is orally bioavailable and readily passes the blood-brain barrier.

LXR-623 Chemical Structure

LXR-623 Chemical Structure

CAS No. 875787-07-8

Purity & Quality Control

LXR-623 Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
THP1 cells Function assay Effect on ABCA1 gene expression in human differentiated THP1 cells, EC50=0.54 μM 19962892
HepG2 cells Function assay Effect on triglyceride accumulation in human HepG2 cells, EC50=1 μM 19962892
HuH7 cells Function assay Agonist activity at human LXRbeta ligand binding domain expressed in human HuH7 cells co-transfected with Gal4-DBD by transactivation assay, EC50=3.67 μM 19962892
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Biological Activity

Description LXR-623 is a novel liver X-receptor(LXR) agonist with IC50 values of 179 nM and 24 nM for LXR-α and LXR-β, respectively. It is orally bioavailable and readily passes the blood-brain barrier.
Targets
LXR-β [1] LXR-α [1]
24 nM 179 nM
In vitro
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[3].
Cell Research Cell lines Human PBMC
Concentrations 2 μM
Incubation Time 18 h
Method 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.
In Vivo
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[1].
Animal Research Animal Models C57/Bl6 mice
Dosages 30 mg/kg
Administration oral administration

Chemical Information & Solubility

Molecular Weight 422.78 Formula

C21H12ClF5N2
CAS No. 875787-07-8 SDF Download LXR-623 SDF
Smiles C1=CC2=C(N(N=C2C(=C1)C(F)(F)F)CC3=C(C=C(C=C3)F)Cl)C4=CC=C(C=C4)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 84 mg/mL ( (198.68 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 84 mg/mL

Water : Insoluble


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In vivo
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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