SR-9243inverse agonist of LXR CAS# 1613028-81-1 |
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Quality Control & MSDS
3D structure
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| 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. |
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| 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. |
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| 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. | ||
| Description | Selective 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
SR-9243 Molarity Calculator
| 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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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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SR9243 is a liver-X-receptor (LXR) inverse agonist that induces LXR-corepressor interaction.
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