SMILES string
O=C(C1CCN(S(=O)(C2=CC=C(C=C2)F)=O)CC1)NC3=NC4=C(S3)C(C)=CC(C)=C4
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear (Warmed)
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
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) that targets an allosteric site distinct from that 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).
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) that targets an allosteric site distinct from that 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).
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Jonah E Zarrow et al.
ACS chemical biology, 18(8), 1891-1904 (2023-08-02)
N-Acyl-phosphatidylethanolamine hydrolyzing phospholipase D (NAPE-PLD) is a zinc metallohydrolase that hydrolyzes N-acyl-phosphatidylethanolamines (NAPEs) to form N-acyl-ethanolamines (NAEs) and phosphatidic acid. Several lines of evidence suggest that reduced NAPE-PLD activity could contribute to cardiometabolic diseases. For instance, NAPEPLD expression is reduced
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