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LXR-623

Cat. No. M6087
LXR-623 Structure
Synonym:

WAY-252623

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM/1mL In DMSO USD 80 In stock
5mg USD 70 In stock
10mg USD 100 In stock
50mg USD 330 In stock
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Quality Control
Biological Activity

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

Protocol
Cell Experiment
Cell lines Human PBMC
Preparation 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.
Concentrations 2 μM
Incubation time 18 h
Animal Experiment
Animal models C57/Bl6 mice
Formulation 0.1% DMSO
Dosages 30 mg/kg
Administration oral
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 422.78
Formula C21H12ClF5N2
CAS Number 875787-07-8
Purity 99.76%
Solubility 84 mg/mL in DMSO
Storage at -20°C
References

An LXR-Cholesterol Axis Creates a Metabolic Co-Dependency for Brain Cancers.
Villa GR, et al. Cancer Cell. 2016 Nov 14;30(5):683-693. PMID: 27746144.

Safety, pharmacokinetics, and pharmacodynamics of single doses of LXR-623, a novel liver X-receptor agonist, in healthy participants.
Katz A, et al. J Clin Pharmacol. 2009 Jun;49(6):643-9. PMID: 19398602.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: LXR-623, WAY-252623 supplier, inhibitors

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