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RO2959 monohydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
RO2959 monohydrochloride图片
CAS NO:2309172-44-7
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
RO2959monohydrochloride是一种有效的选择性CRAC通道抑制剂,IC50为402nM。RO2959monohydrochloride是由Orai1/Stim1通道介导的钙存储进入(SOCE)的有效阻滞剂,IC50为25nM。RO2959monohydrochloride还是人IL-2产生的有效抑制剂,有效阻断T细胞受体触发的基因表达和T细胞功能途径。
Cas No.2309172-44-7
Canonical SMILESO=C(NC1=NC=C(C2=C(C)CCN(C3=NC=C(C)S3)C2)N=C1)C4=C(F)C=CC=C4F.[H]Cl
分子式C21H20ClF2N5OS
分子量463.93
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

RO2959 monohydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM. RO2959 monohydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC50 of 25 nM. RO2959 monohydrochloride is also a potent inhibitor of human IL-2 production, and potently blocks T cell receptor triggered gene expression and T cell functional pathways[1][2].

RO2959 inhibits Orai1 and Orai3 with IC50 values of 25 nM and 530 nM, respectively. RO2959 blocks store operated calcium entry (SOCE) in activated CD4+T lymphocytes with an IC50 value of 265 nM[1].RO2959 is a potent SOCE inhibitor that blocks an IP3-dependent current in CRAC-expressing RBL-2H3 cells and CHO cells stably expressing human Orai1 and Stim1, as well as SOCE in human primary CD4+ T cells triggered by either T cell receptor (TCR) stimulation or thapsigargin treatment. RO2959 completely inhibits cytokine production as well as T cell proliferation mediated by TCR stimulation or MLR (mixed lymphocyte reaction)[1].

[1]. Gang Chen, et al. Characterization of a Novel CRAC Inhibitor That Potently Blocks Human T Cell Activation and Effector Functions. Mol Immunol. 2013 Jul;54(3-4):355-67. [2]. Changbo Zheng, et al. Gastrodin Inhibits Store-Operated Ca 2+ Entry and Alleviates Cardiac Hypertrophy. Front Pharmacol. 2017 Apr 25;8:222.