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

SR9243 Chemical Structure

SR9243 Chemical Structure

CAS No. : 1613028-81-1

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10 mM * 1 mL in DMSO
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Customer Review

Based on 5 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • 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.

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)

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.88%

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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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.

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Product Name:
SR9243
Cat. No.:
HY-16972
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