SR9243 | CAS#1613028-81-1 | LXR inverse agonist

MedKoo Cat#: 407152 | Name: SR9243

Description:

WARNING: This product is for research use only, not for human or veterinary use.

SR9243 is a potent and selective LXR inverse agonist. SR9243 kills cancer cells by inhibiting lipid production and the Warburg effect. SR9243 induces cell death in multiple types of cancer and does not cause the side effects that have derailed previous attempts to target these processes. In cancer cells, SR9243 significantly inhibited the Warburg effect and lipogenesis by reducing glycolytic and lipogenic gene expression. SR9243 induced apoptosis in tumors without inducing weight loss, hepatotoxicity, or inflammation. Malignant cells exhibit aerobic glycolysis (the Warburg effect) and become dependent on de novo lipogenesis, which sustains rapid proliferation and resistance to cellular stress.

Chemical Structure

SR9243

CAS#1613028-81-1

Theoretical Analysis

MedKoo Cat#: 407152

Name: SR9243

CAS#: 1613028-81-1

Chemical Formula: C31H32BrNO4S2

Exact Mass: 625.0956

Molecular Weight: 626.62

Elemental Analysis: C, 59.42; H, 5.15; Br, 12.75; N, 2.24; O, 10.21; S, 10.23

Price and Availability

Size	Price	Availability
10mg	USD 90.00	Ready to ship
25mg	USD 150.00	Ready to ship
50mg	USD 250.00	Ready to ship
100mg	USD 450.00	Ready to ship
200mg	USD 750.00	Ready to ship
500mg	USD 1,250.00	Ready to ship
1g	USD 1,950.00	2 Weeks
2g	USD 3,650.00	2 Weeks
5g	USD 5,650.00	2 Weeks

Bulk Inquiry

Buy Now

Add to Cart

Related CAS #

No Data

Synonym

SR9243; SR-9243; SR 9243.

IUPAC/Chemical Name

N-(3-bromophenethyl)-2,4,6-trimethyl-N-((3'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl)methyl)benzenesulfonamide

InChi Key

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

InChi Code

FYQFEJFTCLKXTQ-UHFFFAOYSA-N

SMILES Code

O=S(C1=C(C)C=C(C)C=C1C)(N(CCC2=CC=CC(Br)=C2)CC3=CC=C(C4=CC=CC(S(=O)(C)=O)=C4)C=C3)=O

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO, DMF, and 4-Methylpyridine

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot# CRB50928

QC Data

View QC data: current batch, Lot# CRB50928

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

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

In vitro activity:

Dual targeting CD133 and LXR is promising for cancer stem cells (CSCs) with dynamic metabolism and self-renewal. SR9243 targeted and eradicated non-CSC tumor cells. Anti-CD133 mAbs-targeted Immunoliposomes (ILipo) for SR9243 delivery into CD133 + CSC is more toxic to CD133 + CSCs than free SR9243, reducing clonogenicity, stemness, and lipogenesis, inducing ROS generation and apoptosis. Reference: Med Oncol. 2023 Apr 24;40(6):156. https://pubmed.ncbi.nlm.nih.gov/37093287/

In vivo activity:

LXR inverse agonists could be therapeutically important in nonalcoholic steatohepatitis (NASH) treatment. Treatment of NASH mice with SR9243 significantly reduced the severity of hepatic inflammation and ameliorated hepatic fibrosis; simultaneously, body weight, serum glucose, and plasma lipid levels were controlled effectively. Reference: Biomed Res Int. 2018 Feb 18;2018:8071093. https://pubmed.ncbi.nlm.nih.gov/29670908/

	Solvent	mg/mL	mM
Solubility
	DMSO	8.4	13.37
	DMF	10.0	15.96
	4-Methylpyridine	20.0	31.92

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 626.62 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Dianat-Moghadam H, Abbasspour-Ravasjani S, Hamishehkar H, Rahbarghazi R, Nouri M. LXR inhibitor SR9243-loaded immunoliposomes modulate lipid metabolism and stemness in colorectal cancer cells. Med Oncol. 2023 Apr 24;40(6):156. doi: 10.1007/s12032-023-02027-4. PMID: 37093287. 2. Dianat-Moghadam H, Khalili M, Keshavarz M, Azizi M, Hamishehkar H, Rahbarghazi R, Nouri M. Modulation of LXR signaling altered the dynamic activity of human colon adenocarcinoma cancer stem cells in vitro. Cancer Cell Int. 2021 Feb 10;21(1):100. doi: 10.1186/s12935-021-01803-4. PMID: 33568147; PMCID: PMC7877018. 3. Huang P, Kaluba B, Jiang XL, Chang S, Tang XF, Mao LF, Zhang ZP, Huang FZ. Liver X Receptor Inverse Agonist SR9243 Suppresses Nonalcoholic Steatohepatitis Intrahepatic Inflammation and Fibrosis. Biomed Res Int. 2018 Feb 18;2018:8071093. doi: 10.1155/2018/8071093. PMID: 29670908; PMCID: PMC5835296. 4. Flaveny CA, Griffett K, El-Gendy Bel-D, Kazantzis M, Sengupta M, Amelio AL, Chatterjee A, Walker J, Solt LA, Kamenecka TM, Burris TP. 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. doi: 10.1016/j.ccell.2015.05.007. Epub 2015 Jun 25. PMID: 26120082; PMCID: PMC4965273.

In vitro protocol:

In vivo protocol:

1. Huang P, Kaluba B, Jiang XL, Chang S, Tang XF, Mao LF, Zhang ZP, Huang FZ. Liver X Receptor Inverse Agonist SR9243 Suppresses Nonalcoholic Steatohepatitis Intrahepatic Inflammation and Fibrosis. Biomed Res Int. 2018 Feb 18;2018:8071093. doi: 10.1155/2018/8071093. PMID: 29670908; PMCID: PMC5835296. 2. Flaveny CA, Griffett K, El-Gendy Bel-D, Kazantzis M, Sengupta M, Amelio AL, Chatterjee A, Walker J, Solt LA, Kamenecka TM, Burris TP. 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. doi: 10.1016/j.ccell.2015.05.007. Epub 2015 Jun 25. PMID: 26120082; PMCID: PMC4965273.

1: Zheng DC, Hu JQ, Mai CT, Huang L, Zhou H, Yu LL, Xie Y. Liver X receptor inverse agonist SR9243 attenuates rheumatoid arthritis via modulating glycolytic metabolism of macrophages. Acta Pharmacol Sin. 2024 Nov;45(11):2354-2365. doi: 10.1038/s41401-024-01315-7. Epub 2024 Jul 10. PMID: 38987388; PMCID: PMC11489696. 2: Cui Y, Yuan X, Zhao Z, Li C, Liu Y, Zhou Y, Zhu Z, Zhang Z. The activation of liver X receptors in Madin-Darby bovine kidney cells and mice restricts infection by bovine viral diarrhea virus. Vet Microbiol. 2024 Jan;288:109948. doi: 10.1016/j.vetmic.2023.109948. Epub 2023 Dec 12. PMID: 38113573. 3: Dianat-Moghadam H, Abbasspour-Ravasjani S, Hamishehkar H, Rahbarghazi R, Nouri M. LXR inhibitor SR9243-loaded immunoliposomes modulate lipid metabolism and stemness in colorectal cancer cells. Med Oncol. 2023 Apr 24;40(6):156. doi: 10.1007/s12032-023-02027-4. PMID: 37093287. 4: Elgendy B, Griffett K, Hegazy L, Di Fruscia P, Sample K, Schoepke E, Kamenecka TM, Burris TP. Synthesis and structure activity relationship of the first class of LXR inverse agonists. Bioorg Chem. 2022 Feb;119:105540. doi: 10.1016/j.bioorg.2021.105540. Epub 2021 Dec 7. PMID: 34902646. 5: Dianat-Moghadam H, Khalili M, Keshavarz M, Azizi M, Hamishehkar H, Rahbarghazi R, Nouri M. Modulation of LXR signaling altered the dynamic activity of human colon adenocarcinoma cancer stem cells in vitro. Cancer Cell Int. 2021 Feb 10;21(1):100. doi: 10.1186/s12935-021-01803-4. PMID: 33568147; PMCID: PMC7877018. 6: Yuan F, Hou L, Wei L, Quan R, Wang J, Liu H, Liu J. Fowl Adenovirus Serotype 4 Induces Hepatic Steatosis via Activation of Liver X Receptor-α. J Virol. 2021 Feb 24;95(6):e01938-20. doi: 10.1128/JVI.01938-20. PMID: 33361420; PMCID: PMC8094942. 7: Toporova L, Grimaldi M, Boulahtouf A, Balaguer P. Assessing the Selectivity of FXR, LXRs, CAR, and RORγ Pharmaceutical Ligands With Reporter Cell Lines. Front Pharmacol. 2020 Jul 24;11:1122. doi: 10.3389/fphar.2020.01122. PMID: 32792956; PMCID: PMC7394005. 8: Li T, Hu SM, Pang XY, Wang JF, Yin JY, Li FH, Wang J, Yang XQ, Xia B, Liu YH, Song WG, Guo SD. The marine-derived furanone reduces intracellular lipid accumulation in vitro by targeting LXRα and PPARα. J Cell Mol Med. 2020 Mar;24(6):3384-3398. doi: 10.1111/jcmm.15012. Epub 2020 Jan 24. Erratum in: J Cell Mol Med. 2024 Nov;28(21):e70108. doi: 10.1111/jcmm.70108. PMID: 31981312; PMCID: PMC7131916. 9: Wu G, Wang Q, Xu Y, Li J, Zhang H, Qi G, Xia Q. Targeting the transcription factor receptor LXR to treat clear cell renal cell carcinoma: agonist or inverse agonist? Cell Death Dis. 2019 May 28;10(6):416. doi: 10.1038/s41419-019-1654-6. PMID: 31138790; PMCID: PMC6538631. 10: Pan YX, Zhuo MQ, Li DD, Xu YH, Wu K, Luo Z. SREBP-1 and LXRα pathways mediated Cu-induced hepatic lipid metabolism in zebrafish Danio rerio. Chemosphere. 2019 Jan;215:370-379. doi: 10.1016/j.chemosphere.2018.10.058. Epub 2018 Oct 10. PMID: 30336314. 11: Huang P, Kaluba B, Jiang XL, Chang S, Tang XF, Mao LF, Zhang ZP, Huang FZ. Liver X Receptor Inverse Agonist SR9243 Suppresses Nonalcoholic Steatohepatitis Intrahepatic Inflammation and Fibrosis. Biomed Res Int. 2018 Feb 18;2018:8071093. doi: 10.1155/2018/8071093. PMID: 29670908; PMCID: PMC5835296. 12: Gui Y, Li A, Zhang J, Li G, Ruan X, Guo Q, Zou W. α-Asarone Alleviated Chronic Constriction Injury-Induced Neuropathic Pain Through Inhibition of Spinal Endoplasmic Reticulum Stress in an Liver X Receptor-Dependent Manner. Anesth Analg. 2018 Sep;127(3):775-783. doi: 10.1213/ANE.0000000000002792. PMID: 29324503. 13: Flaveny CA, Griffett K, El-Gendy Bel-D, Kazantzis M, Sengupta M, Amelio AL, Chatterjee A, Walker J, Solt LA, Kamenecka TM, Burris TP. 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. doi: 10.1016/j.ccell.2015.05.007. Epub 2015 Jun 25. PMID: 26120082; PMCID: PMC4965273.