Page last updated: 2024-12-08

(22r)-22-hydroxycholesterol

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

## (22R)-22-hydroxycholesterol: A Cholesterol Metabolite with Intriguing Biological Activities

(22R)-22-hydroxycholesterol, also known as **22-hydroxycholesterol**, is a **steroid** molecule that is a **metabolite** of cholesterol. It's formed in the body through the action of **cytochrome P450 enzymes** (CYP), specifically CYP46A1.

Here's why (22R)-22-hydroxycholesterol is important for research:

**1. Neurological Function and Brain Health:**

* **Key regulator of brain cholesterol homeostasis:** It plays a crucial role in regulating the levels of cholesterol in the brain, which is essential for normal neuronal function and development.
* **Modulates synaptic activity:** Studies suggest it can affect the function of synapses, the communication points between neurons.
* **Implicated in neurodegenerative diseases:** Elevated levels of 22-hydroxycholesterol have been linked to Alzheimer's disease and other neurodegenerative disorders. Research aims to understand how this metabolite contributes to these diseases and explore potential therapeutic targets.

**2. Immune System Modulation:**

* **Anti-inflammatory effects:** 22-hydroxycholesterol has been shown to have anti-inflammatory properties, potentially by inhibiting the activation of immune cells like macrophages.
* **Modulates immune responses:** It may influence the activity of various immune cells and pathways, contributing to the overall immune response.

**3. Potential Therapeutic Applications:**

* **Drug development for Alzheimer's disease:** Due to its role in brain cholesterol metabolism and its potential to modulate synaptic activity, 22-hydroxycholesterol is a potential target for developing new therapies for Alzheimer's disease.
* **Immune system modulation:** Its anti-inflammatory properties make it an interesting molecule to investigate for potential therapies related to inflammatory diseases.

**4. Key for Understanding Cholesterol Metabolism:**

* **Provides insights into cholesterol pathways:** Studying 22-hydroxycholesterol helps researchers understand the complex pathways of cholesterol metabolism in the body.
* **Unraveling the roles of CYP enzymes:** Research on 22-hydroxycholesterol contributes to our understanding of the functions of specific cytochrome P450 enzymes in the body.

**Challenges and Future Directions:**

* **Complex biological activities:** 22-hydroxycholesterol has multiple and complex effects, making it challenging to fully understand its mechanisms of action and potential therapeutic applications.
* **Further research needed:** More research is needed to investigate its role in various diseases, its interactions with other molecules, and its potential as a therapeutic target.

Overall, (22R)-22-hydroxycholesterol is a fascinating molecule with intriguing biological activities. Further research is crucial to fully understand its role in health and disease and its potential therapeutic applications.

(22R)-22-hydroxycholesterol : An oxysterol that is the 22R-hydroxy derivative of cholesterol. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID167685
CHEMBL ID422904
CHEBI ID67237
SCHEMBL ID103516
MeSH IDM0044609

Synonyms (35)

Synonym
22r-ohc
gtpl2742
chembl422904 ,
(1s,2r,5s,10s,11s,14r,15s)-14-[(2s,3r)-3-hydroxy-6-methylheptan-2-yl]-2,15-dimethyltetracyclo[8.7.0.0;{2,7}.0;{11,15}]heptadec-7-en-5-ol
bdbm20177
17954-98-2
22beta-hydroxycholesterol
(22r)-22-hydroxycholesterol
22(r)-hydroxycholesterol
C05502
cholest-5-en-3beta,22r-diol
22r-hydroxycholesterol
LMST01010086
22(r)-hydroxycholesterol, >=98%
HC9 ,
(3alpha,8alpha,22r)-cholest-5-ene-3,22-diol
chebi:67237 ,
(3s,8s,9s,10r,13s,14s,17r)-17-[(2s,3r)-3-hydroxy-6-methylheptan-2-yl]-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1h-cyclopenta[a]phenanthren-3-ol
cholest-5-ene-3,22-diol, (3beta,22r)-
(3beta,22r)-cholest-5-ene-3,22-diol
(22r)-hydroxycholesterol
(22r)-cholest-5-ene-3beta,22-diol
SCHEMBL103516
(22r)-oh-cholesterol
22-alpha-hydroxycholesterol
5-cholestene-3beta,22(r)-diol
AKOS030254687
22(r)hydroxycholesterol
J-011464
(3s,8s,9s,10r,13s,14s,17r)-17-((2s,3r)-3-hydroxy-6-methylheptan-2-yl)-10,13-dimethyl-2,3,4,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-3-ol
22b-hydroxycholesterol
(8s,9s,10r,13s,14s,17r)-17-((2s,3r)-3-hydroxy-6-methylheptan-2-yl)-10,13-dimethyl-2,3,4,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-3-ol
22alpha-hydroxy cholesterol
DTXSID501313409
PD050577

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" Dose-response curves demonstrated that plasma concentrations observed in clinical trials are sufficient for LXR activation and thus could account for LXR-mediated side-effects such as hypercholesterolemia and hyperlipidemia."( DrugBank screening revealed alitretinoin and bexarotene as liver X receptor modulators.
Achenbach, J; Heitel, P; Merk, D; Moser, D; Proschak, E, 2017
)
0.46
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (3)

ClassDescription
22-hydroxy steroid
oxysterolAn oxygenated derivative of cholesterol
3beta-hydroxy-Delta(5)-steroidAny 3beta-hydroxy-steroid that contains a double bond between positions 5 and 6.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Pathways (15)

PathwayProteinsCompounds
Steroidogenesis1142
Adrenal Hyperplasia Type 3 or Congenital Adrenal Hyperplasia Due to 21-Hydroxylase Deficiency1142
Congenital Lipoid Adrenal Hyperplasia (CLAH) or Lipoid CAH1142
Adrenal Hyperplasia Type 5 or Congenital Adrenal Hyperplasia Due to 17 alpha-Hydroxylase Deficiency1142
17-alpha-Hydroxylase Deficiency (CYP17)1142
11-beta-Hydroxylase Deficiency (CYP11B1)1142
21-Hydroxylase Deficiency (CYP21)1142
Corticosterone Methyl Oxidase I Deficiency (CMO I)1142
Corticosterone Methyl Oxidase II Deficiency (CMO II)1142
Apparent Mineralocorticoid Excess Syndrome1142
3-beta-Hydroxysteroid Dehydrogenase Deficiency1142
Steroid hormone precursor biosynthesis015
superpathway of glycoalkaloid metabolism (Solanaceae)415
solasodine and soladulcidine biosynthesis312
Biochemical pathways: part I0466

Protein Targets (3)

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Nuclear receptor ROR-gammaHomo sapiens (human)EC50 (µMol)0.02000.02000.70359.0000AID1173425; AID1505268
Oxysterols receptor LXR-betaHomo sapiens (human)EC50 (µMol)11.58330.00010.40077.3000AID1458206; AID240210; AID403100
Oxysterols receptor LXR-alphaHomo sapiens (human)EC50 (µMol)6.39330.00010.63026.7100AID101835; AID1458205; AID1797959; AID240218; AID403099; AID758940
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (53)

Processvia Protein(s)Taxonomy
negative regulation of transcription by RNA polymerase IINuclear receptor ROR-gammaHomo sapiens (human)
xenobiotic metabolic processNuclear receptor ROR-gammaHomo sapiens (human)
regulation of glucose metabolic processNuclear receptor ROR-gammaHomo sapiens (human)
regulation of steroid metabolic processNuclear receptor ROR-gammaHomo sapiens (human)
intracellular receptor signaling pathwayNuclear receptor ROR-gammaHomo sapiens (human)
circadian regulation of gene expressionNuclear receptor ROR-gammaHomo sapiens (human)
cellular response to sterolNuclear receptor ROR-gammaHomo sapiens (human)
positive regulation of circadian rhythmNuclear receptor ROR-gammaHomo sapiens (human)
regulation of fat cell differentiationNuclear receptor ROR-gammaHomo sapiens (human)
positive regulation of DNA-templated transcriptionNuclear receptor ROR-gammaHomo sapiens (human)
adipose tissue developmentNuclear receptor ROR-gammaHomo sapiens (human)
T-helper 17 cell differentiationNuclear receptor ROR-gammaHomo sapiens (human)
regulation of transcription by RNA polymerase IINuclear receptor ROR-gammaHomo sapiens (human)
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 (19)

Processvia Protein(s)Taxonomy
RNA polymerase II cis-regulatory region sequence-specific DNA bindingNuclear receptor ROR-gammaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificNuclear receptor ROR-gammaHomo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificNuclear receptor ROR-gammaHomo sapiens (human)
DNA-binding transcription factor activityNuclear receptor ROR-gammaHomo sapiens (human)
protein bindingNuclear receptor ROR-gammaHomo sapiens (human)
oxysterol bindingNuclear receptor ROR-gammaHomo sapiens (human)
zinc ion bindingNuclear receptor ROR-gammaHomo sapiens (human)
ligand-activated transcription factor activityNuclear receptor ROR-gammaHomo sapiens (human)
sequence-specific double-stranded DNA bindingNuclear receptor ROR-gammaHomo sapiens (human)
nuclear receptor activityNuclear receptor ROR-gammaHomo sapiens (human)
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 (8)

Processvia Protein(s)Taxonomy
nucleusNuclear receptor ROR-gammaHomo sapiens (human)
nucleoplasmNuclear receptor ROR-gammaHomo sapiens (human)
nuclear bodyNuclear receptor ROR-gammaHomo sapiens (human)
chromatinNuclear receptor ROR-gammaHomo sapiens (human)
nucleusNuclear receptor ROR-gammaHomo sapiens (human)
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 (44)

Assay IDTitleYearJournalArticle
AID240398Effective concentration against liver X receptor-alpha in HEK293 cell transactivation assay; not calculated as plateau not reached at doses tested2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
Discovery and development of dimeric podocarpic acid leads as potent agonists of liver X receptor with HDL cholesterol raising activity in mice and hamsters.
AID499581Activation of RXR/LXR heterodimer in mouse RAW264.7 cells assessed as induction of ABCA1 mRNA expression by RT-PCR2010Journal of natural products, Aug-27, Volume: 73, Issue:8
Identification of a naturally occurring rexinoid, honokiol, that activates the retinoid X receptor.
AID328046Inhibition of Saccharomyces sp. alpha-glucosidase2008Bioorganic & medicinal chemistry, Apr-15, Volume: 16, Issue:8
Co-existence of alpha-glucosidase-inhibitory and liver X receptor-regulatory activities and their separation by structural development.
AID243328Maximal induction of liver X receptor-alpha receptor in transactivation assay2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
Discovery and development of dimeric podocarpic acid leads as potent agonists of liver X receptor with HDL cholesterol raising activity in mice and hamsters.
AID758940Agonist activity at human LXRalpha-LBD assessed as recruitment of co-activator peptide after 2 hrs by TR-FRET assay2013Bioorganic & medicinal chemistry letters, Jul-15, Volume: 23, Issue:14
Cyanidin, a natural flavonoid, is an agonistic ligand for liver X receptor alpha and beta and reduces cellular lipid accumulation in macrophages and hepatocytes.
AID101844Tested for its ability to activate Liver X receptor-alpha expressed as Relative efficacy determined by maximal increase in relative fluorescence in LiSA2001Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6
Pharmacophore analysis of the nuclear oxysterol receptor LXRalpha.
AID328049Agonist activity at LXR2008Bioorganic & medicinal chemistry, Apr-15, Volume: 16, Issue:8
Co-existence of alpha-glucosidase-inhibitory and liver X receptor-regulatory activities and their separation by structural development.
AID768317Binding affinity to human GFP-tagged NPC1L1 L1072T/L1168I mutant expressed in HEK293 cells assessed as localization to endoplasmic reticulum and plasma membrane at 10 uM after 24 hrs by fluorescence microscopic analysis2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Structure-activity relationship studies of Niemann-Pick type C1-like 1 (NPC1L1) ligands identified by screening assay monitoring pharmacological chaperone effect.
AID1458206Activation of GAL4 fused human LXR beta expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Side-Chain Modified Ergosterol and Stigmasterol Derivatives as Liver X Receptor Agonists.
AID243323Maximal induction of liver X receptor-beta receptor in transactivation assay2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
Discovery and development of dimeric podocarpic acid leads as potent agonists of liver X receptor with HDL cholesterol raising activity in mice and hamsters.
AID403096Displacement of [3H2]F3-methyl AA from human recombinant LXRalpha expressed in Escherichia coli BL21 cells at 100 uM2005Journal of natural products, Aug, Volume: 68, Issue:8
Diterpenoid, steroid, and triterpenoid agonists of liver X receptors from diversified terrestrial plants and marine sources.
AID243990Percent inhibition of [3H2]-F3-methyl AA (1) binding to liver X receptor-alpha at 100 uM2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
Discovery and development of dimeric podocarpic acid leads as potent agonists of liver X receptor with HDL cholesterol raising activity in mice and hamsters.
AID1505268Agonist activity at 6xHis tagged human RORgammat LBD (262 to 507 residues) expressed in Escherichia coli BL21 (DE3) assessed as biotinylated SRC1-2 peptide coactivator recruitment by AlphaScreen assay2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Retinoic Acid Receptor-Related Orphan Receptor γt (RORγt) Agonists as Potential Small Molecule Therapeutics for Cancer Immunotherapy.
AID240397Effective concentration against liver X receptor-beta in HEK293 transactivation assay; not calculated as no plateau obtained at doses tested2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
Discovery and development of dimeric podocarpic acid leads as potent agonists of liver X receptor with HDL cholesterol raising activity in mice and hamsters.
AID1458213Agonist activity at LXR in human HepG2 cells assessed as upregulation of FASN mRNA levels at 10 uM after 6 hrs by qPCR analysis2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Side-Chain Modified Ergosterol and Stigmasterol Derivatives as Liver X Receptor Agonists.
AID240210Effective concentration for cofactor association with recombinant liver X receptor-beta2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
Discovery and development of dimeric podocarpic acid leads as potent agonists of liver X receptor with HDL cholesterol raising activity in mice and hamsters.
AID403364Activity of human recombinant LXRbeta ligand binding domain-mediated transcriptional activity in human HEK293 cells with Gal4 reporter plasmid by luciferase reporter assay2005Journal of natural products, Aug, Volume: 68, Issue:8
Diterpenoid, steroid, and triterpenoid agonists of liver X receptors from diversified terrestrial plants and marine sources.
AID1458222Agonist activity at LXR in human U937 cells assessed as downregulation of LPS-induced TNFalpha mRNA expression at 10 uM after 6 hrs by qPCR analysis2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Side-Chain Modified Ergosterol and Stigmasterol Derivatives as Liver X Receptor Agonists.
AID101835Concentration required for half maximal activity was calculated in human nuclear oxysterol receptor liver X receptor-alpha in LiSA.2001Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6
Pharmacophore analysis of the nuclear oxysterol receptor LXRalpha.
AID1458219Agonist activity at LXR in human U937 cells assessed as upregulation of FASN mRNA levels at 10 uM after 6 hrs by qPCR analysis2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Side-Chain Modified Ergosterol and Stigmasterol Derivatives as Liver X Receptor Agonists.
AID1480585Agonist activity at recombinant human GAL4-DBD-fused LXRalpha-LBD expressed in HEK293T cells at 10 to 20 uM in presence of RXR-antagonist HX531 measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay2017Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
DrugBank screening revealed alitretinoin and bexarotene as liver X receptor modulators.
AID695017Agonist activity at Hh receptor in mouse C3H10T1/2 cells assessed as fold increase in Gli1 expression at 5 uM by RT-PCR analysis relative to control2012ACS medicinal chemistry letters, Oct-11, Volume: 3, Issue:10
Structure-activity relationships for side chain oxysterol agonists of the hedgehog signaling pathway.
AID403098Displacement of [3H2]F3-methyl AA from human recombinant LXRbeta expressed in Escherichia coli BL21 cells at 100 uM2005Journal of natural products, Aug, Volume: 68, Issue:8
Diterpenoid, steroid, and triterpenoid agonists of liver X receptors from diversified terrestrial plants and marine sources.
AID240218Effective concentration for cofactor association with recombinant liver X receptor-alpha2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
Discovery and development of dimeric podocarpic acid leads as potent agonists of liver X receptor with HDL cholesterol raising activity in mice and hamsters.
AID1173425Displacement of [3H]25-hydroxycholesterol from human RORc-LBD expressed in bacterial expression system after 3 hrs by scintillation counting analysis2014Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24
A reversed sulfonamide series of selective RORc inverse agonists.
AID695018Agonist activity at LXR in mouse C3H10T1/2 cells assessed as fold increase in ABCA1 expression at 5 uM by RT-PCR analysis relative to control2012ACS medicinal chemistry letters, Oct-11, Volume: 3, Issue:10
Structure-activity relationships for side chain oxysterol agonists of the hedgehog signaling pathway.
AID1458214Agonist activity at LXR in human HepG2 cells assessed as upregulation of SREBP1c mRNA levels at 10 uM after 6 hrs by qPCR analysis2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Side-Chain Modified Ergosterol and Stigmasterol Derivatives as Liver X Receptor Agonists.
AID403100Agonist activity at human recombinant LXRbeta expressed in Escherichia coli BL21 cells assessed as association of recombinant SRC1 to LXRbeta ligand binding domain by HTRF assay2005Journal of natural products, Aug, Volume: 68, Issue:8
Diterpenoid, steroid, and triterpenoid agonists of liver X receptors from diversified terrestrial plants and marine sources.
AID403360Activity of human recombinant LXRalpha ligand binding domain-mediated transcriptional activity in human HEK293 cells with Gal4 reporter plasmid by luciferase reporter assay2005Journal of natural products, Aug, Volume: 68, Issue:8
Diterpenoid, steroid, and triterpenoid agonists of liver X receptors from diversified terrestrial plants and marine sources.
AID1458220Agonist activity at LXR in human U937 cells assessed as upregulation of ABCA1 mRNA levels at 10 uM after 6 hrs by qPCR analysis2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Side-Chain Modified Ergosterol and Stigmasterol Derivatives as Liver X Receptor Agonists.
AID1458216Agonist activity at LXR in human U937 cells assessed as upregulation of FASN mRNA levels at 10 uM after 16 hrs by qPCR analysis2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Side-Chain Modified Ergosterol and Stigmasterol Derivatives as Liver X Receptor Agonists.
AID499586Agonist activity at RXRalpha in mouse peritoneal macrophages assessed as ApoAI-mediated cholesterol efflux after 24 hrs by Western blotting2010Journal of natural products, Aug-27, Volume: 73, Issue:8
Identification of a naturally occurring rexinoid, honokiol, that activates the retinoid X receptor.
AID1458223Agonist activity at LXR in human HepG2 cells assessed as upregulation of SCD1 mRNA levels at 10 uM after 6 hrs by qPCR analysis2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Side-Chain Modified Ergosterol and Stigmasterol Derivatives as Liver X Receptor Agonists.
AID243986Percent inhibition of [3H2]-F3-methyl AA (1) binding to liver X receptor-beta at 100 uM2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
Discovery and development of dimeric podocarpic acid leads as potent agonists of liver X receptor with HDL cholesterol raising activity in mice and hamsters.
AID1458218Agonist activity at LXR in human U937 cells assessed as upregulation of SREBP1c mRNA levels at 10 uM after 6 hrs by qPCR analysis2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Side-Chain Modified Ergosterol and Stigmasterol Derivatives as Liver X Receptor Agonists.
AID1458205Activation of GAL4 fused human LXR alpha expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Side-Chain Modified Ergosterol and Stigmasterol Derivatives as Liver X Receptor Agonists.
AID1458215Agonist activity at LXR in human U937 cells assessed as upregulation of SCD1 mRNA levels at 10 uM after 16 hrs by qPCR analysis2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Side-Chain Modified Ergosterol and Stigmasterol Derivatives as Liver X Receptor Agonists.
AID403099Agonist activity at human recombinant LXRalpha expressed in Escherichia coli BL21 cells assessed as association of recombinant SRC1 to LXRalpha ligand binding domain by HTRF assay2005Journal of natural products, Aug, Volume: 68, Issue:8
Diterpenoid, steroid, and triterpenoid agonists of liver X receptors from diversified terrestrial plants and marine sources.
AID1458217Agonist activity at LXR in human U937 cells assessed as upregulation of SCD1 mRNA levels at 10 uM after 6 hrs by qPCR analysis relative to control2017Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
Side-Chain Modified Ergosterol and Stigmasterol Derivatives as Liver X Receptor Agonists.
AID1179741Binding affinity to FLAG/tGFP-tagged NPC1 I1061T mutant (unknown origin) expressed in HEK293 cells assessed as localization at 10 uM after 24 hrs by fluorescence microscopy2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Structure-activity relationships of oxysterol-derived pharmacological chaperones for Niemann-Pick type C1 protein.
AID1797959Cell-Free Ligand Sensing Assay (LiSA)-LXRalpha-SRC1 Assay from Article 10.1021/jm0004749: \\Pharmacophore analysis of the nuclear oxysterol receptor LXRalpha.\\2001Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6
Pharmacophore analysis of the nuclear oxysterol receptor LXRalpha.
AID1346993Human Liver X receptor-beta (1H. Liver X receptor-like receptors)1996Nature, Oct-24, Volume: 383, Issue:6602
An oxysterol signalling pathway mediated by the nuclear receptor LXR alpha.
AID1346755Human Liver X receptor-alpha (1H. Liver X receptor-like receptors)1996Nature, Oct-24, Volume: 383, Issue:6602
An oxysterol signalling pathway mediated by the nuclear receptor LXR alpha.
AID1346766Human Farnesoid X receptor (1H. Liver X receptor-like receptors)2006The Journal of pharmacology and experimental therapeutics, Apr, Volume: 317, Issue:1
Oxysterol 22(R)-hydroxycholesterol induces the expression of the bile salt export pump through nuclear receptor farsenoid X receptor but not liver X receptor.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (15)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (6.67)18.2507
2000's5 (33.33)29.6817
2010's9 (60.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 25.48

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 Index25.48 (24.57)
Research Supply Index2.77 (2.92)
Research Growth Index5.17 (4.65)
Search Engine Demand Index23.28 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (25.48)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (6.67%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other14 (93.33%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]