SMALL MOLECULES
Contributor Information
- Name Mario Van Der Stelt
- Institute Leiden University and Leiden University Medical Center
Tool Details
- Tool name: NAPE-Phospholipase D inhibitor (LEI-401) small molecule (tool compound)
- Alternate names: N-acyl phosphatidylethanolamine-specific phospholipase D inhibitor, LEI-41
- Molecular formula: C24H31N5O2
- Tool type: Small molecules
- Tool sub-type: Inhibitor
- Molecular weight of the target: 422
- Application: good bioavailability F (i.p.) = 48 % and brain penetrant. good cellular penetration
- Description: D-type phospholipase that hydrolyzes N-acyl-phosphatidylethanolamines (NAPEs) to produce bioactive N-acylethanolamines/fatty acid ethanolamides (NAEs/FAEs) and phosphatidic acid. Cleaves the terminal phosphodiester bond of diacyl- and alkenylacyl-NAPEs, primarily playing a role in the generation of long-chain saturated and monounsaturated NAEs in the brain._x000D_May control NAPE homeostasis in dopaminergic neuron membranes and regulate neuron survival, partly through RAC1 activation. As a regulator of lipid metabolism in the adipose tissue, mediates the crosstalk between adipocytes, gut microbiota and immune cells to control body temperature and weight. In particular, regulates energy homeostasis by promoting cold-induced brown or beige adipocyte differentiation program to generate heat from fatty acids and glucose. Has limited D-type phospholipase activity toward N-acyl lyso-NAPEs
- Research area: Neurobiology; Metabolism
- Selectivity: IC50> 10uM for CB1R & CB2R, FAAH, PLA2G4E, DAGL, MAGL, ABHD6
- IUPAC: N-(Cyclopropylmethyl)-6-((S)-3-hydroxypyrrolidin-1-yl)-2-((S)-3-phenylpiperidin-1-yl)pyrimidine-4-carboxamide.
- IC50: 27 nM
- Additional notes: Mock et al., Nature Chemical Biology, 2020, 16, 667-675
- For Research Use Only
Target Details
- Target molecular weight: 422
Application Details
- Application: good bioavailability F (i.p.) = 48 % and brain penetrant. good cellular penetration
Handling
- Solubility: 1.7 mg/L
Documentation
- Available on request
Related Tools
References
- • Mock et al. 2021. J Med Chem. 64(1):481-515. PMID: 33382264.
.svg)
.svg)
