质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear (Warmed)
储存温度
2-8°C
SMILES字符串
O=C(C1CCN(S(=O)(C2=CC=C(C=C2)F)=O)CC1)NC3=NC4=C(C)C=CC(C)=C4S3
生化/生理作用
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).
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).
警示用语:
Warning
危险声明
危险分类
Acute Tox. 4 Oral
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°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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