Compounds > sr9238
Page last updated: 2024-11-13

sr9238

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Description

SR9238: liver-selective LXR inverse agonist that suppresses hepatic steatosis; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID71478195
CHEMBL ID4284414
SCHEMBL ID15773678
MeSH IDM000600738

Synonyms (17)

Synonym
SCHEMBL15773678
ethyl 5-[[[4-(3-methylsulfonylphenyl)phenyl]methyl-(2,4,6-trimethylphenyl)sulfonylamino]methyl]furan-2-carboxylate
sr9238
gtpl8692
sr 9238
1416153-62-2
ethyl 5-[[[[3'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]methyl][(2,4,6-trimethylphenyl)sulfonyl]amino]methyl]-2-furancarboxylate
AKOS027470306
EX-A3559
ethyl 5-(((2,4,6-trimethyl-n-((3'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl)methyl)phenyl)sulfonamido)methyl)furan-2-carboxylate
HY-101442
CS-0021352
BS-15090
Q27088868
D80447
CHEMBL4284414 ,
bdbm50465712

Research Excerpts

Actions

ExcerptReferenceRelevance
"SR9238 displays high potency for both LXRα and LXRβ (40-200 nM IC50) and was designed to display liver specificity so as to avoid potential side effects due to suppression of LXR in the periphery."( A liver-selective LXR inverse agonist that suppresses hepatic steatosis.
Burris, TP; El-Gendy, Bel-D; Griffett, K; Kamenecka, TM; Solt, LA, 2013)		1.11
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Oxysterols receptor LXR-betaHomo sapiens (human)IC50 (µMol)0.07150.00790.92859.9000AID1414115; AID1743596
Oxysterols receptor LXR-betaHomo sapiens (human)Ki0.35200.00220.07300.3520AID1562690
Oxysterols receptor LXR-alphaHomo sapiens (human)IC50 (µMol)0.18700.00901.06049.9000AID1414116; AID1743594
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (43)

Processvia Protein(s)Taxonomy
hormone-mediated signaling pathwayOxysterols receptor LXR-betaHomo sapiens (human)
negative regulation of macrophage derived foam cell differentiationOxysterols receptor LXR-betaHomo sapiens (human)
positive regulation of triglyceride biosynthetic processOxysterols receptor LXR-betaHomo sapiens (human)
positive regulation of cholesterol effluxOxysterols receptor LXR-betaHomo sapiens (human)
positive regulation of lipid storageOxysterols receptor LXR-betaHomo sapiens (human)
negative regulation of cholesterol storageOxysterols receptor LXR-betaHomo sapiens (human)
intracellular receptor signaling pathwayOxysterols receptor LXR-betaHomo sapiens (human)
negative regulation of lipid transportOxysterols receptor LXR-betaHomo sapiens (human)
positive regulation of cholesterol transportOxysterols receptor LXR-betaHomo sapiens (human)
phosphatidylcholine acyl-chain remodelingOxysterols receptor LXR-betaHomo sapiens (human)
cholesterol homeostasisOxysterols receptor LXR-betaHomo sapiens (human)
mRNA transcription by RNA polymerase IIOxysterols receptor LXR-betaHomo sapiens (human)
positive regulation of fatty acid biosynthetic processOxysterols receptor LXR-betaHomo sapiens (human)
negative regulation of proteolysisOxysterols receptor LXR-betaHomo sapiens (human)
negative regulation of DNA-templated transcriptionOxysterols receptor LXR-betaHomo sapiens (human)
positive regulation of DNA-templated transcriptionOxysterols receptor LXR-betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIOxysterols receptor LXR-betaHomo sapiens (human)
negative regulation of pinocytosisOxysterols receptor LXR-betaHomo sapiens (human)
positive regulation of lipoprotein lipase activityOxysterols receptor LXR-betaHomo sapiens (human)
positive regulation of protein metabolic processOxysterols receptor LXR-betaHomo sapiens (human)
negative regulation of type II interferon-mediated signaling pathwayOxysterols receptor LXR-betaHomo sapiens (human)
positive regulation of high-density lipoprotein particle assemblyOxysterols receptor LXR-betaHomo sapiens (human)
positive regulation of pancreatic juice secretionOxysterols receptor LXR-betaHomo sapiens (human)
positive regulation of secretion of lysosomal enzymesOxysterols receptor LXR-betaHomo sapiens (human)
negative regulation of cold-induced thermogenesisOxysterols receptor LXR-betaHomo sapiens (human)
positive regulation of miRNA transcriptionOxysterols receptor LXR-betaHomo sapiens (human)
negative regulation of response to endoplasmic reticulum stressOxysterols receptor LXR-betaHomo sapiens (human)
cell differentiationOxysterols receptor LXR-betaHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIOxysterols receptor LXR-betaHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIOxysterols receptor LXR-alphaHomo sapiens (human)
hormone-mediated signaling pathwayOxysterols receptor LXR-alphaHomo sapiens (human)
negative regulation of macrophage derived foam cell differentiationOxysterols receptor LXR-alphaHomo sapiens (human)
positive regulation of triglyceride biosynthetic processOxysterols receptor LXR-alphaHomo sapiens (human)
positive regulation of cholesterol effluxOxysterols receptor LXR-alphaHomo sapiens (human)
negative regulation of cholesterol storageOxysterols receptor LXR-alphaHomo sapiens (human)
intracellular receptor signaling pathwayOxysterols receptor LXR-alphaHomo sapiens (human)
negative regulation of lipid transportOxysterols receptor LXR-alphaHomo sapiens (human)
positive regulation of cholesterol transportOxysterols receptor LXR-alphaHomo sapiens (human)
positive regulation of transporter activityOxysterols receptor LXR-alphaHomo sapiens (human)
response to progesteroneOxysterols receptor LXR-alphaHomo sapiens (human)
positive regulation of toll-like receptor 4 signaling pathwayOxysterols receptor LXR-alphaHomo sapiens (human)
phosphatidylcholine acyl-chain remodelingOxysterols receptor LXR-alphaHomo sapiens (human)
cholesterol homeostasisOxysterols receptor LXR-alphaHomo sapiens (human)
regulation of circadian rhythmOxysterols receptor LXR-alphaHomo sapiens (human)
mRNA transcription by RNA polymerase IIOxysterols receptor LXR-alphaHomo sapiens (human)
negative regulation of macrophage activationOxysterols receptor LXR-alphaHomo sapiens (human)
apoptotic cell clearanceOxysterols receptor LXR-alphaHomo sapiens (human)
positive regulation of fatty acid biosynthetic processOxysterols receptor LXR-alphaHomo sapiens (human)
negative regulation of proteolysisOxysterols receptor LXR-alphaHomo sapiens (human)
positive regulation of DNA-templated transcriptionOxysterols receptor LXR-alphaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIOxysterols receptor LXR-alphaHomo sapiens (human)
positive regulation of lipid biosynthetic processOxysterols receptor LXR-alphaHomo sapiens (human)
negative regulation of pinocytosisOxysterols receptor LXR-alphaHomo sapiens (human)
negative regulation of inflammatory responseOxysterols receptor LXR-alphaHomo sapiens (human)
positive regulation of lipoprotein lipase activityOxysterols receptor LXR-alphaHomo sapiens (human)
positive regulation of protein metabolic processOxysterols receptor LXR-alphaHomo sapiens (human)
lipid homeostasisOxysterols receptor LXR-alphaHomo sapiens (human)
sterol homeostasisOxysterols receptor LXR-alphaHomo sapiens (human)
negative regulation of type II interferon-mediated signaling pathwayOxysterols receptor LXR-alphaHomo sapiens (human)
triglyceride homeostasisOxysterols receptor LXR-alphaHomo sapiens (human)
cellular response to lipopolysaccharideOxysterols receptor LXR-alphaHomo sapiens (human)
negative regulation of pancreatic juice secretionOxysterols receptor LXR-alphaHomo sapiens (human)
negative regulation of secretion of lysosomal enzymesOxysterols receptor LXR-alphaHomo sapiens (human)
negative regulation of cold-induced thermogenesisOxysterols receptor LXR-alphaHomo sapiens (human)
negative regulation of response to endoplasmic reticulum stressOxysterols receptor LXR-alphaHomo sapiens (human)
cell differentiationOxysterols receptor LXR-alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (14)

Processvia Protein(s)Taxonomy
RNA polymerase II cis-regulatory region sequence-specific DNA bindingOxysterols receptor LXR-betaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificOxysterols receptor LXR-betaHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificOxysterols receptor LXR-betaHomo sapiens (human)
DNA bindingOxysterols receptor LXR-betaHomo sapiens (human)
protein bindingOxysterols receptor LXR-betaHomo sapiens (human)
zinc ion bindingOxysterols receptor LXR-betaHomo sapiens (human)
chromatin DNA bindingOxysterols receptor LXR-betaHomo sapiens (human)
apolipoprotein A-I receptor bindingOxysterols receptor LXR-betaHomo sapiens (human)
nuclear retinoid X receptor bindingOxysterols receptor LXR-betaHomo sapiens (human)
ATPase bindingOxysterols receptor LXR-betaHomo sapiens (human)
nuclear receptor activityOxysterols receptor LXR-betaHomo sapiens (human)
transcription cis-regulatory region bindingOxysterols receptor LXR-alphaHomo sapiens (human)
transcription cis-regulatory region bindingOxysterols receptor LXR-alphaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificOxysterols receptor LXR-alphaHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificOxysterols receptor LXR-alphaHomo sapiens (human)
DNA bindingOxysterols receptor LXR-alphaHomo sapiens (human)
nuclear receptor activityOxysterols receptor LXR-alphaHomo sapiens (human)
protein bindingOxysterols receptor LXR-alphaHomo sapiens (human)
zinc ion bindingOxysterols receptor LXR-alphaHomo sapiens (human)
cholesterol bindingOxysterols receptor LXR-alphaHomo sapiens (human)
chromatin DNA bindingOxysterols receptor LXR-alphaHomo sapiens (human)
sterol response element bindingOxysterols receptor LXR-alphaHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingOxysterols receptor LXR-alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (7)

Processvia Protein(s)Taxonomy
nucleusOxysterols receptor LXR-betaHomo sapiens (human)
nucleoplasmOxysterols receptor LXR-betaHomo sapiens (human)
cytoplasmOxysterols receptor LXR-betaHomo sapiens (human)
cytosolOxysterols receptor LXR-betaHomo sapiens (human)
RNA polymerase II transcription regulator complexOxysterols receptor LXR-betaHomo sapiens (human)
chromatinOxysterols receptor LXR-betaHomo sapiens (human)
nucleusOxysterols receptor LXR-betaHomo sapiens (human)
nucleusOxysterols receptor LXR-alphaHomo sapiens (human)
nucleoplasmOxysterols receptor LXR-alphaHomo sapiens (human)
cytoplasmOxysterols receptor LXR-alphaHomo sapiens (human)
cytosolOxysterols receptor LXR-alphaHomo sapiens (human)
RNA polymerase II transcription regulator complexOxysterols receptor LXR-alphaHomo sapiens (human)
chromatinOxysterols receptor LXR-alphaHomo sapiens (human)
receptor complexOxysterols receptor LXR-alphaHomo sapiens (human)
nucleusOxysterols receptor LXR-alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (10)

Assay IDTitleYearJournalArticle
AID1562690Binding affinity to recombinant human LXRbeta-LBD expressed in Escherichia coli BL21 (DE3) assessed as inhibitory constant incubated for 30 mins by fluorescence polarization binding assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Identify liver X receptor β modulator building blocks by developing a fluorescence polarization-based competition assay.
AID1743594Inverse agonist activity at human LXRalpha transfected in human HEK293T cells co-transfected with pSG5 and pGL3/(DR-4)-c-fos-FF-luc/pCMV/Renilla-luc assessed as receptor transactivation incubated for 20 hrs by dual luciferase reporter gene assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Discovery of novel liver X receptor inverse agonists as lipogenesis inhibitors.
AID1743595Inverse agonist activity at human LXRalpha transfected in human HEK293T cells co-transfected with pSG5 and pGL3/(DR-4)-c-fos-FF-luc/pCMV/Renilla-luc assessed as receptor transactivation incubated for 20 hrs by dual luciferase reporter gene assay relative 2020European journal of medicinal chemistry, Nov-15, Volume: 206Discovery of novel liver X receptor inverse agonists as lipogenesis inhibitors.
AID1743596Inverse agonist activity at human LXRbeta transfected in human HEK293T cells co-transfected with pSG5 and pGL3/(DR-4)-c-fos-FF-luc/pCMV/Renilla-luc assessed as receptor transactivation incubated for 20 hrs by dual luciferase reporter gene assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Discovery of novel liver X receptor inverse agonists as lipogenesis inhibitors.
AID1414115Inverse agonist activity at LXRbeta (unknown origin) expressed in HEK293 cells 24 hrs by Dual-Glo luciferase assay2018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Recent Advances in the Medicinal Chemistry of Liver X Receptors.
AID1743597Inverse agonist activity at human LXRbeta transfected in human HEK293T cells co-transfected with pSG5 and pGL3/(DR-4)-c-fos-FF-luc/pCMV/Renilla-luc assessed as receptor transactivation incubated for 20 hrs by dual luciferase reporter gene assay relative t2020European journal of medicinal chemistry, Nov-15, Volume: 206Discovery of novel liver X receptor inverse agonists as lipogenesis inhibitors.
AID1414116Inverse agonist activity at LXRalpha (unknown origin) expressed in HEK293 cells 24 hrs by Dual-Glo luciferase assay2018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Recent Advances in the Medicinal Chemistry of Liver X Receptors.
AID1414122Reduction in hepatic collagen deposition in mouse at 30 mg/kg, ip for 30 days2018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Recent Advances in the Medicinal Chemistry of Liver X Receptors.
AID1346765Mouse Liver X receptor-alpha (1H. Liver X receptor-like receptors)2013ACS chemical biology, Mar-15, Volume: 8, Issue:3
A liver-selective LXR inverse agonist that suppresses hepatic steatosis.
AID1346776Mouse Liver X receptor-beta (1H. Liver X receptor-like receptors)2013ACS chemical biology, Mar-15, Volume: 8, Issue:3
A liver-selective LXR inverse agonist that suppresses hepatic steatosis.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (7)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's4 (57.14)24.3611
2020's3 (42.86)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 20.12

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index20.12 (24.57)
Research Supply Index2.08 (2.92)
Research Growth Index4.56 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (20.12)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (14.29%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other6 (85.71%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
fenofibrate
Pharmavit: a polyvitamin product, comprising vitamins A, D2, B1, B2, B6, C, E, nicotinamide, & calcium pantothene; may be a promising agent for application to human populations exposed to carcinogenic and genetic hazards of ionizing radiation; RN from CHEMLINE		2.2510aromatic ether;
chlorobenzophenone;
isopropyl ester;
monochlorobenzenes		antilipemic drug;
environmental contaminant;
geroprotector;
xenobiotic
4-chlorophenol
4-chlorophenol: used as a root canal irrigant. 4-chlorophenol : A monochlorophenol substituted at the pare position by a chlorine atom.		2.2110monochlorophenol
butylparaben
[no description available]		2.2110organic molecular entity
3-chlorophenol
3-chlorophenol : A monochlorophenol carrying the chloro substituent at position 3.		2.2110monochlorophenol
indazoles
Indazoles: A group of heterocyclic aromatic organic compounds consisting of the fusion of BENZENE and PYRAZOLES.		2.2510indazole
4-phenoxyphenol
[no description available]		2.2110phenoxyphenol
bis(4-oxyphenyl)sulfide
4,4'-thiodiphenol: structure in first source		2.2110phenols
4-ethylphenol
4-ethylphenol: RN given refers to parent cpd. 4-ethylphenol : A member of the class of phenols carrying an ethyl substituent at position 4.		2.2110phenolsfungal xenobiotic metabolite
2-ethoxybenzoic acid
[no description available]		2.2110
2-chloro-1,4-dimethoxybenzene
[no description available]		2.2110dimethoxybenzene
gw 3965
GW 3965: a liver X receptor ligand		2.6320diarylmethane
t0901317
T0901317: an LXRalpha and LXRbeta agonist		2.6320
way 252623
2-(2-chloro-4-fluorobenzyl)-3-(4-fluorophenyl)-7-(trifluoromethyl)-2H-indazole: a partial LXR agonist		2.6320
cholenic acid dimethylamide
cholenic acid dimethylamide: binds LXRalpha receptor; structure in first source		3.2710
incb-018424
[no description available]		2.2110nitrile;
pyrazoles;
pyrrolopyrimidine		antineoplastic agent;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
sr9243
SR9243: an LXR inverse agonist; structure in first source. SR9243 : A sulfonamide resulting from the formal condensation of the sulfonic acid group of mesitylene-2-sulphonic acid with the amino group of 2-(m-bromophenyl)ethylamine in which the nitrogen is substituted by a 4-[m-(methylsulfonyl)phenyl]benzyl group.		2.4110bromobenzenes;
sulfonamide;
sulfone		antineoplastic agent;
apoptosis inducer;
liver X receptor inverse agonist
ConditionIndicatedRelationship StrengthStudiesTrials
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.5120
Liver Steatosis
[description not available]		02.0810
Fatty Liver
Lipid infiltration of the hepatic parenchymal cells resulting in a yellow-colored liver. The abnormal lipid accumulation is usually in the form of TRIGLYCERIDES, either as a single large droplet or multiple small droplets. Fatty liver is caused by an imbalance in the metabolism of FATTY ACIDS.		02.0810
Atherogenesis
[description not available]		03.0910
Atherosclerosis
A thickening and loss of elasticity of the walls of ARTERIES that occurs with formation of ATHEROSCLEROTIC PLAQUES within the ARTERIAL INTIMA.		03.0910
Hepatitis B Virus Infection
[description not available]		02.2510
Hepatitis B
INFLAMMATION of the LIVER in humans caused by a member of the ORTHOHEPADNAVIRUS genus, HEPATITIS B VIRUS. It is primarily transmitted by parenteral exposure, such as transfusion of contaminated blood or blood products, but can also be transmitted via sexual or intimate personal contact.		02.2510
Fatty Liver, Nonalcoholic
[description not available]		02.1310
Non-alcoholic Fatty Liver Disease
Fatty liver finding without excessive ALCOHOL CONSUMPTION.		02.1310