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Merck
CN

SML2164

Sigma-Aldrich

Bepristat 1a

≥98% (HPLC)

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别名:
1-[(3-Chloro-4-hydroxyphenyl)methyl]-N-ethyl-N-methyl-4-(2-phenoxyethyl)-4-piperidinecarboxamide
经验公式(希尔记法):
C24H31ClN2O3
分子量:
430.97
UNSPSC代码:
12352200
NACRES:
NA.77

检测方案

≥98% (HPLC)

形式

powder

颜色

white to light brown

溶解性

DMSO: 2 mg/mL, clear

储存温度

2-8°C

SMILES字符串

ClC1=C(O)C=CC(CN2CCC(C(N(CC)C)=O)(CCOC3=CC=CC=C3)CC2)=C1

生化/生理作用

Bepristat 1a is a selective reversible inhibitor of protein disulfide isomerase (PDI), an enzyme in the endoplasmic reticulum that catalyzes disulfide bond breakage and reformation to catalyze protein folding. Unlike most PDI inhibitors, Bepristat 1a binds at the substrate-binding site, rather than the catalytic site. It blocked PDI activity with an IC50 value of 700 nM. PDI is up-regulated in several cancers, has been implicated in neurodegenerative processes, and plays an important role in thrombus formation. Bepristat 1a potently inhibited platelet aggregation and thrombus formation in vivo.

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


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Roelof H Bekendam et al.
Nature communications, 7, 12579-12579 (2016-08-31)
Protein disulfide isomerase (PDI) is an oxidoreductase essential for folding proteins in the endoplasmic reticulum. The domain structure of PDI is a-b-b'-x-a', wherein the thioredoxin-like a and a' domains mediate disulfide bond shuffling and b and b' domains are substrate

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