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Merck
CN

529531

PICK1 PDZ结构域抑制剂,FSC231

The PICK1 PDZ Domain Inhibitor, FSC231 controls the biological activity of PICK1. This small molecule/inhibitor is primarily used for Neuroscience applications.

别名:

PICK1 PDZ结构域抑制剂,FSC231, (E)-乙基-2-氰基-3-(3,4-二氯苯基)丙烯酰基氨基甲酸酯

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关于此项目

经验公式(希尔记法):
C13H10Cl2N2O3
分子量:
313.14
NACRES:
NA.77
UNSPSC Code:
12352200
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产品名称

PICK1 PDZ结构域抑制剂,FSC231, The PICK1 PDZ Domain Inhibitor, FSC231 controls the biological activity of PICK1. This small molecule/inhibitor is primarily used for Neuroscience applications.

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

off-white

solubility

DMSO: 100 mg/mL

shipped in

ambient

storage temp.

2-8°C

Quality Level

Other Notes

Thorsen, T.S., et al. 2010.Proc.Natl.Acad.Sci. USA107, 413.

Packaging

用惰性气体包装

Preparation Note

复溶后,等分并冷冻保存(-20°C)。储备溶液在-20°C下可稳定保存至多6个月。

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

毒性:监管审查(Z)

General description

一种可渗透细胞的丙烯酰氨基甲酸酯化合物,可选择性靶向PICK1(蛋白与C激酶1相互作用)的PDZ(PSD-95/Discs-large/ZO-1同源性)结构域,但不靶向PSD-95(突触后密度蛋白95)的PDZ结构域和GRIP1(谷氨酸受体相互作用蛋白1),可有效竞争多巴胺转运蛋白/DAT(竞争性结合测定中Ki ~10 µM),GluR2(竞争性结合测定中Ki ~10 µM)和mRluR7a(使用来自50 µM FSC231处理的HEK293的裂解物通过Co-IP抑制〜70%),与PICK1 PDZ结合的C末端。显示在NMDR诱导的大鼠海马神经元内在化后(有和没有50µ M FSC231处理下t1/2=7.5 vs 10分钟)可加速GluR2表面再循环,并预防鼠海马切片中的LTD(有和没有50 µM FSC231处理下长期抑制%=74 vs 50)和LTP(有和没有50 µM FSC231处理下长期增强%=137 vs 266)。

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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Qian Dou et al.
BioMed research international, 2021, 9884297-9884297 (2021-07-27)
We performed in vitro and in vivo experiments to explore the role of protein kinase C-binding protein 1 (PICK1), an intracellular transporter involved in oxidative stress-related neuronal diseases, in sepsis-related acute kidney injury (AKI). Firstly, PCR, western blotting, and immunohistochemistry
Zengyan Zhu et al.
Psychopharmacology, 240(1), 239-248 (2022-12-24)
Muscarinic acetylcholine receptors (mAChRs) have been shown to play significant roles in the regulation of normal cognitive processes in the hippocampus, and α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors (AMPARs) are also involved in these processes. This study aims to explore the mAChR-mediated regulation

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