#160829

NAPE-Phospholipase D inhibitor (LEI-401) small molecule (tool compound)

Cat. #160829

NAPE-Phospholipase D inhibitor (LEI-401) small molecule (tool compound)

Cat. #: 160829

Sub-type: Inhibitor

Availability: Please enquire for quantities and pricing

Application: good bioavailability F (i.p.) = 48 % and brain penetrant. good cellular penetration

This fee is applicable only for non-profit organisations. If you are a for-profit organisation or a researcher working on commercially-sponsored academic research, you will need to contact our licensing team for a commercial use license.

Contributor

Inventor: Mario Van Der Stelt

Institute: Leiden University and Leiden University Medical Center

Tool Details
Target Details
Application Details
References

Tool Details

*FOR RESEARCH USE ONLY

  • Tool name: NAPE-Phospholipase D inhibitor (LEI-401) small molecule (tool compound)
  • Alternate name: N-acyl phosphatidylethanolamine-specific phospholipase D inhibitor, LEI-41
  • Molecular formula: C24H31N5O2
  • Tool sub type: Inhibitor
  • 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
  • Application: good bioavailability F (i.p.) = 48 % and brain penetrant. good cellular penetration
  • 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.
  • Molecular weight: 422
  • Solubility: 1.7 mg/L
  • Additional notes: Mock et al., Nature Chemical Biology, 2020, 16, 667-675

Target Details

  • Ic50: 27 nM

Application Details

  • Application: good bioavailability F (i.p.) = 48 % and brain penetrant. good cellular penetration

References

  • Mock et al. 2021. J Med Chem. 64(1):481-515. PMID: 33382264.