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SR-9243

inverse agonist of LXR CAS# 1613028-81-1

SR-9243

Catalog No. BCC3983----Order now to get a substantial discount!

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Quality Control of SR-9243

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Chemical structure

SR-9243

3D structure

Chemical Properties of SR-9243

Cas No. 1613028-81-1 SDF Download SDF
PubChem ID 76073169 Appearance Powder
Formula C31H32BrNO4S2 M.Wt 626.62
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 20 mg/mL (31.92 mM; Need ultrasonic)
Chemical Name N-[2-(3-bromophenyl)ethyl]-2,4,6-trimethyl-N-[[4-(3-methylsulfonylphenyl)phenyl]methyl]benzenesulfonamide
SMILES CC1=CC(=C(C(=C1)C)S(=O)(=O)N(CCC2=CC(=CC=C2)Br)CC3=CC=C(C=C3)C4=CC(=CC=C4)S(=O)(=O)C)C
Standard InChIKey FYQFEJFTCLKXTQ-UHFFFAOYSA-N
Standard InChI InChI=1S/C31H32BrNO4S2/c1-22-17-23(2)31(24(3)18-22)39(36,37)33(16-15-25-7-5-9-29(32)19-25)21-26-11-13-27(14-12-26)28-8-6-10-30(20-28)38(4,34)35/h5-14,17-20H,15-16,21H2,1-4H3
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of SR-9243

DescriptionSelective LXR inverse agonist. Exhibits no significant activity at other nuclear receptors at maximally effective concentration. Inhibits the Warburg effect and lipogenesis by down-regulation of LXR-mediated gene expression. Selectively reduces cell viability and induces apoptosis in cancer cell lines in vitro. Suppresses hepatic steatosis and inhibits growth of tumor xenografts in mice.

SR-9243 Dilution Calculator

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SR-9243 Molarity Calculator

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Preparing Stock Solutions of SR-9243

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.5959 mL 7.9793 mL 15.9586 mL 31.9173 mL 39.8966 mL
5 mM 0.3192 mL 1.5959 mL 3.1917 mL 6.3835 mL 7.9793 mL
10 mM 0.1596 mL 0.7979 mL 1.5959 mL 3.1917 mL 3.9897 mL
50 mM 0.0319 mL 0.1596 mL 0.3192 mL 0.6383 mL 0.7979 mL
100 mM 0.016 mL 0.0798 mL 0.1596 mL 0.3192 mL 0.399 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on SR-9243

SR9243 is a liver-X-receptor (LXR) inverse agonist that induces LXR-corepressor interaction. It potently reduces cancer cell viability (IC50=15–104 nM) in MTT reduction assays in prostate (PC3 and DU-145), colorectal (SW620 and HT29), and lung (HOP-62 and NCI-H23) cancer cell lines. [1]

LXR (liver X receptor) is a member of the nuclear receptor family of transcription factors. It is an important regulator of glycolysis and lipogenesis enzyme expression.

In SW620 cells, 1 mM SR9243 treatment for 12 hours induces cell death with a robust increase in caspase 3/7 activation. In addition, SR9243 disrupts the Warburg effect, suppresses lipogenesis gene expression and lipid production in cancer cells without effecting normal cells. [1]

In colon tumor xenograft, SR9243 substantially and dose-dependently reduces tumor growth, glycolytic (GCK1, PFK2, PFK1 and LDH) and lipogenic (SCD1, FASN, and SREBP1c) enzyme expression without promoting weight loss. SR9243 also blocks tumor growth without causing immune or hepatic toxicity in vivo. [1]

Reference:
1.  Flaveny CA, Griffett K, El-Gendy Bel-D et al. Broad Anti-tumor Activity of a Small Molecule that Selectively Targets the Warburg Effect and Lipogenesis. Cancer Cell. 2015 Jul 13;28(1):42-56.

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Description

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

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