1. Metabolic Enzyme/Protease
  2. LXR
  3. LXR-623

LXR-623 (Synonyms: WAY 252623)

Cat. No.: HY-10629 Purity: 99.40%
Handling Instructions

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

For research use only. We do not sell to patients.

LXR-623 Chemical Structure

LXR-623 Chemical Structure

CAS No. : 875787-07-8

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10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
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10 mg USD 90 In-stock
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50 mg USD 360 In-stock
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100 mg USD 640 In-stock
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200 mg USD 940 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

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

    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.
    • Biological Activity

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    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]

    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].

    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].

    Clinical Trial
    Molecular Weight

    422.78

    Formula

    C₂₁H₁₂ClF₅N₂

    CAS No.

    875787-07-8

    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 47 mg/mL (111.17 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    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.
    References
    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.

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

    References
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    LXR-623
    Cat. No.:
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