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Merck
CN

SML4089

VU534

≥98% (HPLC)

别名:

N-(5,7-Dimethyl-2-benzothiazolyl)-1-[(4-fluorophenyl)sulfonyl]-4-piperidinecarboxamide, VU 534, VU-534

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关于此项目

经验公式(希尔记法):
C21H22FN3O3S2
化学文摘社编号:
分子量:
447.55
MDL编号:
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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(S3)C(C)=CC(C)=C4

生化/生理作用

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).

象形图

Exclamation mark

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

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历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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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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