VU534 is a NAPE-PLD activator, with an EC50 of 0.30 μM. VU534 is dual inhibitors of FAAH and sEH (IC50 of 1.2 μM). VU534 increases efferocytosis in a NAPE-PLD dependent manner. VU534 has the potential for cardiometabolic diseases study [1] .
VU534 (up to 30 μM, 24 h) shows minimal cytotoxicity in HepG2 and Raw264.7 cell lines [1].
VU534 (3-30 μM, 1 h) increases NAPE-PLD activity in Raw264.7 cells [1].
VU534 (1 h) increases NAPE-PLD activity in HepG2 cells, with the EC50 values of 1.5 μM[1].
VU534 (5 μM, 1 h) increases NAPE-PLD activity 1.5-fold, but not reverses LEI-401-inhibited NAPE-PLD activity [1].
VU534 (10 μM, 6 h) significantly enhances efferocytosis in bone-marrow-derived macrophages, but not work in Napepld-/- KO[1].
References:
[1]. Jonah E Zarrow, et al. Small Molecule Activation of NAPE-PLD Enhances Efferocytosis by Macrophages. ACS Chem. Biol. 2023, 18, 8, 1891–1904.