Page last updated: 2024-11-13

sar127303

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

Description

SAR127303: inhibits monoacylglycerol lipase; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID54761543
CHEMBL ID4215558
SCHEMBL ID14834237
MeSH IDM000611292

Synonyms (9)

Synonym
SCHEMBL14834237
bdbm50450707
CHEMBL4215558 ,
rlymqnqychgicp-uhfffaoysa-n
1,1,1,3,3,3-hexafluoropropan-2-yl 4-[[(4-chlorophenyl)sulfonylamino]methyl]piperidine-1-carboxylate
1352011-38-1
AKOS040746321
sar127303
PD193826

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" CPD-4645 (10 mg/kg, subcutaneously) or vehicle was dosed 1 and 7 h after status epilepticus onset in video-electroencephalography (EEG) recorded mice."( Inhibition of monoacylglycerol lipase terminates diazepam-resistant status epilepticus in mice and its effects are potentiated by a ketogenic diet.
Butler, CR; Guilmette, E; Pauletti, A; Piro, JR; Porcu, L; Rizzi, M; Salamone, A; Samad, TA; Sheehan, MJ; Terrone, G; Vezzani, A; Villa, BR, 2018
)
0.48
[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)
Monoglyceride lipaseMus musculus (house mouse)IC50 (µMol)0.00380.00010.08360.5200AID1363919
Monoglyceride lipaseHomo sapiens (human)IC50 (µMol)0.02900.00091.126810.0000AID1363896
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (11)

Processvia Protein(s)Taxonomy
lipid metabolic processMonoglyceride lipaseHomo sapiens (human)
fatty acid biosynthetic processMonoglyceride lipaseHomo sapiens (human)
inflammatory responseMonoglyceride lipaseHomo sapiens (human)
regulation of signal transductionMonoglyceride lipaseHomo sapiens (human)
arachidonic acid metabolic processMonoglyceride lipaseHomo sapiens (human)
triglyceride catabolic processMonoglyceride lipaseHomo sapiens (human)
acylglycerol catabolic processMonoglyceride lipaseHomo sapiens (human)
regulation of inflammatory responseMonoglyceride lipaseHomo sapiens (human)
regulation of sensory perception of painMonoglyceride lipaseHomo sapiens (human)
monoacylglycerol catabolic processMonoglyceride lipaseHomo sapiens (human)
regulation of endocannabinoid signaling pathwayMonoglyceride lipaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (4)

Processvia Protein(s)Taxonomy
lysophospholipase activityMonoglyceride lipaseHomo sapiens (human)
protein bindingMonoglyceride lipaseHomo sapiens (human)
protein homodimerization activityMonoglyceride lipaseHomo sapiens (human)
acylglycerol lipase activityMonoglyceride lipaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (4)

Processvia Protein(s)Taxonomy
endoplasmic reticulum membraneMonoglyceride lipaseHomo sapiens (human)
cytosolMonoglyceride lipaseHomo sapiens (human)
plasma membraneMonoglyceride lipaseHomo sapiens (human)
membraneMonoglyceride lipaseHomo sapiens (human)
membraneMonoglyceride lipaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (2)

Assay IDTitleYearJournalArticle
AID1363919Inhibition of mouse MAGL2017Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
Therapeutic Potential of Fatty Acid Amide Hydrolase, Monoacylglycerol Lipase, and N-Acylethanolamine Acid Amidase Inhibitors.
AID1363896Inhibition of human MAGL2017Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
Therapeutic Potential of Fatty Acid Amide Hydrolase, Monoacylglycerol Lipase, and N-Acylethanolamine Acid Amidase Inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's5 (100.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (20.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other4 (80.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]