2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. LXR
  4. LXR-623

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

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 66 In-stock
Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Solid
1 mg USD 30 In-stock
5 mg USD 60 In-stock
10 mg USD 95 In-stock
50 mg USD 340 In-stock
100 mg USD 560 In-stock
200 mg USD 910 In-stock
500 mg   Get quote  
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Customer Review

Based on 10 publication(s) in Google Scholar

LXR-623 Related Antibodies

Top Publications Citing Use of Products

    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.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    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].

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

    LXR-623 Related Antibodies
    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.
    Clinical Trial
    Molecular Weight

    422.78

    Formula

    C21H12ClF5N2
    CAS No.
    Appearance

    Solid

    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
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 47 mg/mL (111.17 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" 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
    View the Complete Stock Solution Preparation Table

    * 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.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

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

    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.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • 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:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.48%

    COA (256 KB) LCMS (92 KB)

    Handling Instructions (2659 KB)
    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

    Complete Stock Solution Preparation Table

    * 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.

    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
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    LXR-623 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    LXR-623875787-07-8WAY 252623LXR623LXR 623WAY252623WAY-252623LXRLiver X receptorInhibitorinhibitorinhibit

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