2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. LXR
  4. SR9243

SR9243 is a liver-X-receptor (LXR) inverse agonist that induces LXR-corepressor interaction.

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

CAS No. : 1613028-81-1

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Based on 7 publication(s) in Google Scholar

SR9243 Related Antibodies

Top Publications Citing Use of Products

    SR9243 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2019 May 28;10(6):416.   [Abstract]

    CCK8 assays were used to detect the difference in viability of ccRCC cells (786-O and ACHN) after 48, 72 and 96 h of treatment with different doses of SR9243.

    SR9243 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2019 May 28;10(6):416.   [Abstract]

    786-O cells treated with 0.1 µM SR9243 or 1 µM LXR623 for 72 h by EdU assay.

    SR9243 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2019 May 28;10(6):416.   [Abstract]

    786-O and ACHN cells were stained with Annexin-V FITC/PI and analysed via flow cytometry. SR9243 (0.1 µM) and LXR623 (1 µM for 786-O cells, 5 µM for ACHN cells) acted on the two cell lines.

    SR9243 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2019 May 28;10(6):416.   [Abstract]

    Western blotting experiments were performed by treating three groups of cells with DMSO, 0.1 µM SR9243 or LXR623 (786-O, 0.1 µM; ACHN, 1 µM) for 48 h and then extracting proteins. The protein levels of Bax, Bcl2, and Cleaved-Caspase3 were determined via immunoblotting.

    SR9243 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2019 May 28;10(6):416.   [Abstract]

    qRT-PCR showed differences in mRNA levels of SREBP1, FASN and SCD1 48 h after treatment of cells with SR9243.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    SR9243 is a liver-X-receptor (LXR) inverse agonist that induces LXR-corepressor interaction.

    In Vitro

    SR9243 specifically targets LXR and downregulates LXR-mediated gene expression, dose-dependently suppresses LXRα- and LXRβ-dependent transcription at nanomolar concentrations, and potently inhibits LXR-driven luciferase activity in cultured cancer cells. SR9243 potently reduces cancer cell viability at nanomolar concentrations (IC50 appr 15-104 nM) in prostate (PC3 and!DU-145), colorectal (SW620 and HT29), and lung (HOP-62 and NCI-H23) cancer cell lines. And the colony-forming capacity of cancer cells is also significantly loared by SR9243 in a dose-dependent manner. SR9243 is a potent inhibitor of lipogenic gene expression that selectively kills cancer cells by depleting intracellular lipids. Combination of cancer cell media with oleate, stearate, and palmitate in combination completely rescues cancer cell viability in cancer cells. Fatty acid supplementation also rescues the viability of SW620 cells in which glycolysis is substantially disrupted[1].

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

    SR9243 Related Antibodies
    In Vivo

    SR9243 is able to profoundly inhibit tumor glycolysis, lipogenesis, and induce apoptotic cancer cell death without promoting weight loss in vivo. SR9243 inhibits tumor growth without profoundly repressing glycolytic gene expression, and inhibits tumor growth and lipogenesis without hepatotoxicity or inflammation in vivo[1].

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

    626.62

    Formula

    C31H32BrNO4S2
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    BrC1=CC(CCN(S(C2=C(C)C=C(C)C=C2C)(=O)=O)CC(C=C3)=CC=C3C4=CC(S(=O)(C)=O)=CC=C4)=CC=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 : 20 mg/mL (31.92 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.5959 mL 7.9793 mL 15.9586 mL
    5 mM 0.3192 mL 1.5959 mL 3.1917 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
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    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

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    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    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (3.99 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  15% Cremophor EL    85% Saline

      Solubility: 10 mg/mL (15.96 mM); Suspended solution; Need ultrasonic

    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
    References
    Cell Assay
    [1]

    Cancer cells are plated at low-density (5×103) cells per well. Cells are then treated with either DMSO vehicle control, SR9243 (100 nM) or SR9243 (10 μM) and allowed to grow for 4 days. Colonies are then fixed with Formaldehyde (1%) and stained with Crystal violet solution (0.05% w/v)[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mice[1]
    C57BL/6J, Nu/Nu and Ob/Ob mice are used in the assay. Mice are housed in sterile ventilated cages, fed a standard diet, and provided water ad libitum. Mice are treated after two weeks of acclimation. Mice are monitored daily for signs of illness, pain, or severe weight loss. All mice are humanely euthanized using CO2 followed by cervical dislocation. For liver lipid content analysis 8-week old male Ob/Ob mice are fed a high fat diet (60% kcal/fat, 20% carbohydrate) for the duration of the experiment and are treated with vehicle or SR9243 for 3 days. Mice are injected (i.p.) with either vehicle (10% DMSO, 10% Tween-80) or SR9243 (30 mg/kg) once daily[1].

    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 1.5959 mL 7.9793 mL 15.9586 mL 39.8966 mL
    5 mM 0.3192 mL 1.5959 mL 3.1917 mL 7.9793 mL
    10 mM 0.1596 mL 0.7979 mL 1.5959 mL 3.9897 mL
    15 mM 0.1064 mL 0.5320 mL 1.0639 mL 2.6598 mL
    20 mM 0.0798 mL 0.3990 mL 0.7979 mL 1.9948 mL
    25 mM 0.0638 mL 0.3192 mL 0.6383 mL 1.5959 mL
    30 mM 0.0532 mL 0.2660 mL 0.5320 mL 1.3299 mL
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    SR9243 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:

    SR92431613028-81-1SR 9243SR-9243LXRLiver X receptorInhibitorinhibitorinhibit

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