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Biochem/physiol Actions
Allosteric site-targeting, reversible, potent and selective N-Acyl-phosphatidylethanolamine-hydrolyzing phospholipase D (NAPE-PLD) activator.
VU533 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/2.6-fold, human EC50/Emax = 0.2 μM/1.9-fold, using respective recombinant NAPE-PLD) that targets an allosteric site distinct from that of PE, DCA, or LEI-401, showing only little potency toward FAAH and sEH. VU533 enhances murine BMDMs efferocytosis (by 1.53-fold with 6h 10 μM pretreatment) by activating cellular NAPE-PLD activity (EC50/Emax = 2.5 μM/2.2-fold in RAW264.7 and 3.0 μM/1.6-fold in HepG2).
| Quality Level | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear (Warmed) |
| storage temp. | 2-8°C |
| SMILES string | O=C(C1CCN(S(=O)(C2=CC=C(C=C2)F)=O)CC1)NC3=NC4=C(C)C=CC(C)=C4S3 |
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