Cat. No.: HY-10629

LXR-623

(Synonyms: WAY 252623)

14 Cited Publications

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Based on 14 publication(s) in Google Scholar

LXR-623 is a brain-penetrant partial LXRα and full LXRβ agonist, with IC₅₀s of 24 nM and 179 nM, respectively.

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Pureté: 99.95%
CAS No.: 875787-07-8
Formule: C₂₁H₁₂ClF₅N₂
Masse moléculaire:422.78

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

LXR-623 Chemical Structure

CAS No.: 875787-07-8

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (14)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

LXR-623 is a brain-penetrant partial LXRα and full LXRβ agonist, with IC₅₀s of 24 nM and 179 nM, respectively.

IC₅₀ & Target

IC50: 24 nM (LXR-α), 179 nM (LXR-β)^[2]^[3]

Cellular Effect

Cell Line	Type	Value	Description	References
A 172	IC₅₀	8.3 μM Compound: LXR-623	Antiproliferative activity against human A 172 cells measured after 7 days by CCK8 assay Antiproliferative activity against human A 172 cells measured after 7 days by CCK8 assay	[PMID: 32248003]
HEK-293T	EC₅₀	0.9 μM Compound: 6; WAY252623	Partial agonist activity at recombinant human GAL4-DBD-fused LXRbeta-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay Partial agonist activity at recombinant human GAL4-DBD-fused LXRbeta-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay	[PMID: 28169169]
HEK-293T	EC₅₀	1.44 μM Compound: 6; WAY252623	Partial agonist activity at recombinant human GAL4-DBD-fused LXRalpha-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay Partial agonist activity at recombinant human GAL4-DBD-fused LXRalpha-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay	[PMID: 28169169]
HepG2	EC₅₀	1 μM Compound: 4 (WAY-252623)	Effect on triglyceride accumulation in human HepG2 cells Effect on triglyceride accumulation in human HepG2 cells	[PMID: 19962892]
HepG2	EC₅₀	1911 nM Compound: 12, WAY-252623	Effect on triglyceride accumulation in human HepG2 cells Effect on triglyceride accumulation in human HepG2 cells	[PMID: 18973288]
HepG2	EC₅₀	2114 nM Compound: 12, WAY-252623	Effect on SREBP1c gene expression in human HepG2 cells Effect on SREBP1c gene expression in human HepG2 cells	[PMID: 18973288]
Huh-7	EC₅₀	3.67 μM Compound: 12, WAY-252623	Agonist activity at human recombinant LXRbeta ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay Agonist activity at human recombinant LXRbeta ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay	[PMID: 18973288]
Huh-7	EC₅₀	3.67 μM Compound: 4 (WAY-252623)	Agonist activity at human LXRbeta ligand binding domain expressed in human HuH7 cells co-transfected with Gal4-DBD by transactivation assay Agonist activity at human LXRbeta ligand binding domain expressed in human HuH7 cells co-transfected with Gal4-DBD by transactivation assay	[PMID: 19962892]
Huh-7	EC₅₀	6.66 μM Compound: 12, WAY-252623	Agonist activity at human recombinant LXRalpha ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay Agonist activity at human recombinant LXRalpha ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay	[PMID: 18973288]
Huh-7	EC₅₀	6.66 μM Compound: 4 (WAY-252623)	Agonist activity at human LXRalpha ligand binding domain expressed in human HuH7 cells co-transfected with Gal4-DBD by transactivation assay Agonist activity at human LXRalpha ligand binding domain expressed in human HuH7 cells co-transfected with Gal4-DBD by transactivation assay	[PMID: 19962892]
THP-1	EC₅₀	0.54 μM Compound: 4 (WAY-252623)	Effect on ABCA1 gene expression in human differentiated THP1 cells Effect on ABCA1 gene expression in human differentiated THP1 cells	[PMID: 19962892]
THP-1	EC₅₀	1275 nM Compound: 12, WAY-252623	Stimulation of [3H]cholesterol efflux in human THP1 foam cells loaded with ac-LDL Stimulation of [3H]cholesterol efflux in human THP1 foam cells loaded with ac-LDL	[PMID: 18973288]
THP-1	EC₅₀	541 nM Compound: 12, WAY-252623	Effect on ABCA1 gene expression in human differentiated THP1 cells Effect on ABCA1 gene expression in human differentiated THP1 cells	[PMID: 18973288]
U-251	IC₅₀	3.06 μM Compound: LXR-623	Antiproliferative activity against human U-251 cells measured after 7 days by CCK8 assay Antiproliferative activity against human U-251 cells measured after 7 days by CCK8 assay	[PMID: 32248003]
U-87MG ATCC	IC₅₀	6.14 μM Compound: LXR-623	Antiproliferative activity against human U87 cells overexpressing EGFR variant III measured after 7 days by CCK8 assay Antiproliferative activity against human U87 cells overexpressing EGFR variant III measured after 7 days by CCK8 assay	[PMID: 32248003]

In Vitro

LXR-623 potently kills U87EGFRvIII and GBM39 cells in vitro while completely sparing NHAs. LXR-623 also increases ABCA1 protein and decreases LDLR protein levels in all three cell lines. LXR-623 suppresses LDLR expression, increases expression of the ABCA1 efflux transporter, and induces substantial cell death in all of the GBM samples tested. LXR-623 (5 μM) also induces GBM cell death through activation of LXRβ^[1]. LXR-623 treatment of human PBMC in vitro significantly increases transcription of ABCA1 and ABCG1^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

LXR-623 (400 mg/kg, p.o.) crosses the blood-brain barrier, induces target gene expression, and achieves therapeutic levels in GBM cells in the brain with minimal activity in the periphery. LXR-623 inhibits tumor growth, promotes tumor cell death, and prolongs the survival of mice bearing intracranial patient-derived GBMs^[1]. LXR-623 (1.5, 5 mg/kg/day) significantly reduces progression of atherosclerosis in animals compared with the placebo group^[2]. WAY-252623 (15 and 50 mg/kg) results in a significant reduction of atherosclerosis in a dose-dependent manner. WAY-252623 (20, 60, and 120 mg/kg/day, p.o.) displays neutral lipid effects in this CETP-expressing Syrian hamster^[3]. Moreover, LXR-623 (50 mg/kg) induces gene expression in rodent peripheral blood cells in rat. LXR-623 (0, 15 and 50 mg/kg) dose-dependently upregulates transcription of ABCA1 and ABCG1 in monkey whole blood cells proportional to dose^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 875787-07-8
Appearance Solid
Masse moléculaire 422.78
Formule C₂₁H₁₂ClF₅N₂
Color White to off-white
SMILES

ClC1=C(CN2N=C(C(C(F)(F)F)=CC=C3)C3=C2C4=CC=C(F)C=C4)C=CC(F)=C1
Synonyms

WAY 252623
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (14)

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Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
J Exp Clin Cancer Res

Oncolytic adenovirus encoding apolipoprotein A1 suppresses metastasis of triple-negative breast cancer in mice. [Abstract]

2024 Apr 3;43(1):102. PMID: 38566092
Cell Death Dis

Targeting the transcription factor receptor LXR to treat clear cell renal cell carcinoma: agonist or inverse agonist?. [Abstract]

2019 May 28;10(6):416. PMID: 31138790
Cell Death Dis

The LXR-623-induced long non-coding RNA LINC01125 suppresses the proliferation of breast cancer cells via PTEN/AKT/p53 signaling pathway. [Abstract]

2019 Mar 13;10(3):248. PMID: 30867411

LXR-623 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2019 Mar 13;10(3):248. [Abstract]

Western blotting analysis is used to determine the effect of LXR-623 (5 μM) and LINC01125 on PTEN, AKT, p-AKT, MDM2, p-MDM2, and p53 expression levels in MDA-MB-231 and BT-549 cells.
Life Sci

MicroRNA-325 facilitates atherosclerosis progression by mediating the SREBF1/LXR axis via KDM1A. [Abstract]

2021 Jul 15:277:119464. PMID: 33811891
One Health Adv

2026 Apr 10;4(1):7.
Nutrients

Endoplasmic Reticulum Stress Affects Cholesterol Homeostasis by Inhibiting LXRα Expression in Hepatocytes and Macrophages. [Abstract]

2020 Oct 11;12(10):3088. PMID: 33050595
Int J Mol Sci

The Effect of Cholesterol Efflux on Endothelial Dysfunction Caused by Oxidative Stress. [Abstract]

2023 Mar 21;24(6):5939. PMID: 36983012
J Virol

The cholesterol transporter Niemann-Pick C1 facilitates the entry of porcine epidemic diarrhea coronavirus. [Abstract]

2026 Jun 9:e0030126. PMID: 42262129
Metabolites

2-Hydroxypropyl-β-cyclodextrin Regulates the Epithelial to Mesenchymal Transition in Breast Cancer Cells by Modulating Cholesterol Homeostasis and Endoplasmic Reticulum Stress. [Abstract]

2021 Aug 23;11(8):562. PMID: 34436503
Viruses

Pseudorabies Virus Inhibits Expression of Liver X Receptors to Assist Viral Infection. [Abstract]

2022 Mar 3;14(3):514. PMID: 35336921
SSRN

2025 Aug 13.
bioRxiv

Cholesterol-mediated Lysosomal Dysfunction in APOE4 Astrocytes Promotes α-Synuclein Pathology in Human Brain Tissue. [Abstract]

2025 Feb 14:2025.02.09.637107. PMID: 39975381
Radboud University Nijmegen

2021 Mar.

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (236.53 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3653 mL

11.8265 mL

23.6530 mL

5 mM

0.4731 mL

2.3653 mL

4.7306 mL

10 mM

0.2365 mL

1.1826 mL

2.3653 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.91 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.91 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocole

Animal Administration^[1]

Five-week-old female athymic nu/nu mice are used in the experiment. A total of 1×10⁵ U87EGFRvIII IRFP720 or GBM39 IRFP720 cells in 5 μL of PBS is intracranially injected into the mouse brain. Tumors are allowed to establish over the course of 7-10 days and engraftment of tumors is quantitatively confirmed via FMT signal intensity. Tumor growth is monitored using an FMT 2500 fluorescence tomography system. For drug treatment studies, vehicle (0.5% methylcellulose, 2% Tween 80 in water) or LXR-623 (400 mg/kg) resuspended in vehicle are administered to mice via oral gavage daily starting at day 7 postinjection.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (282 KB)
SDS (480 KB)
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- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Villa GR, et al. An LXR-Cholesterol Axis Creates a Metabolic Co-Dependency for Brain Cancers. Cancer Cell. 2016 Nov 14;30(5):683-693. [Content Brief]

[2]. Giannarelli C, et al. Synergistic effect of liver X receptor activation and simvastatin on plaque regression and stabilization: an magnetic resonance imaging study in a model of advanced atherosclerosis. Eur Heart J. 2012 Jan;33(2):264-73. [Content Brief]

[3]. Quinet EM, et al. LXR ligand lowers LDL cholesterol in primates, is lipid neutral in hamster, and reduces atherosclerosis in mouse. J Lipid Res. 2009 Dec;50(12):2358-70. [Content Brief]

[4]. DiBlasio-Smith EA, et al. Discovery and implementation of transcriptional biomarkers of synthetic LXR agonists in peripheral blood cells. J Transl Med. 2008 Oct 16;6:59. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3653 mL	11.8265 mL	23.6530 mL	59.1324 mL
	5 mM	0.4731 mL	2.3653 mL	4.7306 mL	11.8265 mL
	10 mM	0.2365 mL	1.1826 mL	2.3653 mL	5.9132 mL
	15 mM	0.1577 mL	0.7884 mL	1.5769 mL	3.9422 mL
	20 mM	0.1183 mL	0.5913 mL	1.1826 mL	2.9566 mL
	25 mM	0.0946 mL	0.4731 mL	0.9461 mL	2.3653 mL
	30 mM	0.0788 mL	0.3942 mL	0.7884 mL	1.9711 mL
	40 mM	0.0591 mL	0.2957 mL	0.5913 mL	1.4783 mL
	50 mM	0.0473 mL	0.2365 mL	0.4731 mL	1.1826 mL
	60 mM	0.0394 mL	0.1971 mL	0.3942 mL	0.9855 mL
	80 mM	0.0296 mL	0.1478 mL	0.2957 mL	0.7392 mL
	100 mM	0.0237 mL	0.1183 mL	0.2365 mL	0.5913 mL

Keywords

LXR-623

14 Cited Publications

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LXR-623

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

CNS-Penetrant Compound Library

Anti-Cardiovascular Disease Compound Library

Chemical Probe Library

Lipid Metabolism Compound Library

Targeted Diversity Library

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Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) LXR-623

Activité biologique

Chemical Information

Publications (14)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

LXR-623

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

CNS-Penetrant Compound Library

Anti-Cardiovascular Disease Compound Library

Chemical Probe Library

Lipid Metabolism Compound Library

Targeted Diversity Library

Human Metabolite Library

Nuclear Receptor Compound Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) LXR-623

Activité biologique

Chemical Information

Publications (14)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

LXR-623 Related Classifications

HY-10629 Related Classifications