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LXR-623

Catalog No. T1783 CAS 875787-07-8

Synonyms: LXR623, WAY 252623

LXR-623 (WAY 252623) is an orally bioavailable and highly specifical synthetic modulator of LXR.

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LXR-623, CAS 875787-07-8

Pack Size	Availability	Price/USD
5 mg	In stock	$ 47.00
10 mg	In stock	$ 72.00
25 mg	In stock	$ 148.00
50 mg	In stock	$ 258.00
100 mg	In stock	$ 463.00
1 mL * 10 mM (in DMSO)	In stock	$ 52.00

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Purity: 99.24%

Purity: 97.91%

Purity: 97.17%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	LXR-623 (WAY 252623) is an orally bioavailable and highly specifical synthetic modulator of LXR.
Targets&IC50	LXRβ:24 nM, LXRα:179 nM
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].
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].
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)

Synonyms	LXR623, WAY 252623
Molecular Weight	422.78
Formula	C21H12ClF5N2
CAS No.	875787-07-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 42.3 mg/mL (100 mM)

Ethanol: 42.3 mg/mL (100 mM)

References and Literature

1. Katz A, et al. J Clin Pharmacol. 2009, 49(6):643-9. 2. Elizabeth A DiBlasio-Smith, et al. Journal of Translational Medicine. 2008, 6:59. 3. Villa GR, et al. Cancer Cell. 2016, 30(5):683-693.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Anti-Metabolism Disease Compound Library Fluorochemical Library Clinical Compound Library Anti-Cardiovascular Disease Compound Library Metabolism Compound Library Bioactive Lipid Compound Library Bioactive Compounds Library Max Nuclear Receptor Compound Library Bioactive Compound Library

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Keywords

LXR-623 875787-07-8 Metabolism Liver X Receptor Inhibitor Liver X receptor WAY-252623 LXR LXR623 inhibit WAY 252623 LXR 623 WAY252623 inhibitor

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