SML2164
Bepristat 1a
≥98% (HPLC)
别名:
1-[(3-Chloro-4-hydroxyphenyl)methyl]-N-ethyl-N-methyl-4-(2-phenoxyethyl)-4-piperidinecarboxamide
产品名称
Bepristat 1a, ≥98% (HPLC)
InChI key
AYJKPBTXOIHUFT-UHFFFAOYSA-N
SMILES string
ClC1=C(O)C=CC(CN2CCC(C(N(CC)C)=O)(CCOC3=CC=CC=C3)CC2)=C1
assay
≥98% (HPLC)
form
powder
color
white to light brown
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Biochem/physiol Actions
Selective reversible inhibitor of protein disulfide isomerase (PDI)
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.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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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