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CRAC Channel Inhibitor IV, GSK-7975A-CAS 1253186-56-9-Calbiochem

品牌
Sigma-Aldrich
CAS
1253186-56-9
货号
5.34351
包装型号
规格纯度
价格
2309.64 *本价格含增值税费
促销
服务
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  • 包邮
  • 增值税票
数量
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半岛bd体育手机客户端 名称:
1253186-56-9
CRAC Channel Inhibitor IV, GSK-7975A-CAS 1253186-56-9-Calbiochem
2,6-Difluoro-N-(1-(4-hydroxy-2-(trifluoromethyl)benzyl)-1H-pyrazol-3-yl)benzamide, CRAC Chanel Blocker, GSK-7975A, GSK7975A
半岛bd体育手机客户端 介绍:

半岛bd体育手机客户端 说明

一般描述

A cell permeable pyrazol derivative that acts as a specific CRAC (Ca2+release-activated Ca2+entry) channel blocker (IC50= 800 nM in RBL cells) possibly downstream of STIM1 oligomerization and STIM1/Orail interaction. Shown to fully block Orail1 and at 10 ?M in HeK293 cells (t1/2= 75-100 s), but with 2.5-fold slower than La3+ kinetically. Also inhibits Orail3 currents with similar potency but with faster kinetics (t1/2= ~20s). Exhibits good selectivity against a panel of more than 16 ion channels, only with reduced effects on L-type Ca2+(CaV1.2) and TRPV6 channels. Inhibits store-operated Ca2+ entry (IC50= 3.4 ?M) at 10 ?M in normal pancreatic acinar cells, but not in pancreatic acinar cell line AR42J which has a neuronal phenotype and hepatocytes, and does not affect acetylcholine or cholecystokinin induced Ca2+spiking. Shown to block palmitoleic acid ethyl ester-induced trysin and protease activitiest and abolish necrosis. Additionally, reduces Fc?RI-dependent Ca2+influx, at 3 ?M and reduces the release of histamine, leukotriene C4, and cytokines (IL-5/-8/-13 and TNFα) by up to 50% in human lung mast cells (HLMC) and from rat, mouse and guinea-pig preparations.

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
A cell permeable pyrazol derivative that acts as a specific CRAC (Ca2+release-activated Ca2+entry) channel blocker (IC50= 800 nM in RBL cells) possibly downstream of STIM1 oligomerization and STIM1/Orail interaction. Shown to fully block Orail1 and at 10 ?M in HeK293 cells (t1/2= 75-100 s), but with 2.5-fold slower than La3+ kinetically. Also inhibits Orail3 currents with similar potency but with faster kinetics (t1/2= ~20s). Exhibits good selectivity against a panel of more than 16 ion channels, only with reduced effects on L-type Ca2+(CaV1.2) and TRPV6 channels. Inhibits store-operated Ca2+ entry (IC50= 3.4 ?M) at 10 ?M in normal pancreatic acinar cells, but not in pancreatic acinar cell line AR42J which has a neuronal phenotype and hepatocytes, and does not affect acetylcholine or cholecystokinin induced Ca2+spiking. Shown to block palmitoleic acid ethyl ester-induced trysin and protease activitiest and abolish necrosis. Additionally, reduces Fc?RI-dependent Ca2+influx, at 3 ?M and reduces the release of histamine, leukotriene C4, and cytokines (IL-5/-8/-13 and TNFα) by up to 50% in human lung mast cells (HLMC) and from rat, mouse and guinea-pig preparations.

生化/生理作用

Cell permeable: yes
Primary Target
CRAC
Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

Voronina, S., et al. 2015.Biochem. J.465,405.
Derler, I., et al. 2013.Cell Calcium.53,139l.
Gerasimenko, J.V., et al. 2013.PNAS.110,13186.
Louise, V., et al. 2013.Eur. J. Pharmacol.704,49.

Ashmole, I., et al. 2012.J. Aller. Clin. Immun.129,1628.

法律信息

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

基本信息

经验(实验)分子式 C18H12F5N3O2
分子量 397.30

半岛bd体育手机客户端 性质

质量水平 100
测定 ≥98% (HPLC)
形式 solid
manufacturer/tradename Calbiochem?
储存条件 OK to freeze
protect from light
颜色 off-white
溶解性 DMSO: 50 mg/mL
储存温度 ?20℃

安全信息

储存分类代码 11 - Combustible Solids
WGK WGK 3
闪点(F) Not applicable
闪点(C) Not applicable

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