N-(5,7-Dimethyl-2-benzothiazolyl)-1-[(4-fluorophenyl)sulfonyl]-4-piperidinecarboxamide

Biological Activity

Allosteric site-targeting, reversible, potent and selective N-Acyl-phosphatidylethanolamine-hydrolyzing phospholipase D (NAPE-PLD) activator.

VU534 is a non-cytotoxic (up to 30 μM in murine RAW264.7 and human HepG2 cultures), reversible, potent and selective N-Acyl-phosphatidylethanolamine-hydrolyzing phospholipase D activator (mouse EC50/Emax = 0.30 μM/2.1-fold, human EC50/Emax = 0.93 μM/1.8-fold, using respective recombinant NAPE-PLD) th at targets an allosteric site distinct from th at of PE, DCA, or LEI-401, showing only weak sEH inhibition (IC50/Emax = 1.2 μM/55%) and little potency toward FAAH. VU534 enhances murine BMDMs efferocytosis (by 1.65-fold with 6h 10 μM pretreatment) by activating cellular NAPE-PLD activity (EC50/Emax = 6.6 μM/1.6-fold in RAW264.7 and 1.5 μM/1.6-fold in HepG2).