VU534

VU534 is an activator of N-acyl-phosphatidylethanolamine-hydrolyzing phospholipase D (NAPE-PLD), which hydrolyzes NAPEs into N-acyl ethanolamines (NAEs) and phosphatidic acid. It increases NAPE-PLD activity in cell-free assays (EC50s = 0.3 and 0.93 µM for the recombinant mouse and human enzymes, respectively). VU534 (20 µM) also increases NAPE-PLD activity in RAW 264.7 cells, an effect that can be blocked by the NAPE-PLD inhibitor bithionol (Cay-21844), and in HepG2 cells (EC50 = 1.5 µM). It also inhibits soluble epoxide hydrolase (sEH) with a maximal inhibition of 55% and weakly inhibits fatty acid amide hydrolase (FAAH). VU534 (10 µM) increases efferocytosis in isolated wild-type mouse bone marrow-derived macrophages (BMDMs) but not in BMDMs isolated from Napepld-/- mice.Formal Name: N-(5,7-dimethyl-2-benzothiazolyl)-1-[(4-fluorophenyl)sulfonyl]-4-piperidinecarboxamide. CAS Number: 923509-20-0. Synonyms: N-Acyl-Phosphatidylethanolamine-Hydrolysing Phospholipase D Activator 534, NAPE-PLD Activator 534. Molecular Formula: C21H22FN3O3S2. Formula Weight: 447.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble: >10 mg/ml, Methanol: Slightly Soluble: 0.1-1 mg/ml. SMILES: CC1=CC(C)=C2C(N=C(NC(C3CCN(S(=O)(C4=CC=C(F)C=C4)=O)CC3)=O)S2)=C1. InChi Code: InChI=1S/C21H22FN3O3S2/c1-13-11-14(2)19-18(12-13)23-21(29-19)24-20(26)15-7-9-25(10-8-15)30(27,28)17-5-3-16(22)4-6-17/h3-6,11-12,15H,7-10H2,1-2H3,(H,23,24,26). InChi Key: RLHUIVPGYWWIQZ-UHFFFAOYSA-N.