RO2959 monohydrochloride 是一种有效的选择性CRAC通道抑制剂，IC50为 402 nM。RO2959 monohydrochloride 是由Orai1/Stim1通道介导的钙存储进入 (SOCE) 的有效阻滞剂，IC50为 25 nM。RO2959 monohydrochloride 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。

RO2959 monohydrochloride is a potent and selective CRAC channel inhibitor with an IC 50 of 402 nM. RO2959 monohydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC 50 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 IC 50 values of 25 nM and 530 nM, respectively. RO2959 blocks store operated calcium entry (SOCE) in activated CD4+T lymphocytes with an IC 50 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].

2309172-44-7

C21H20ClF2N5OS

463.93

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years