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 |
Sigma-Aldrich