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| | RO2959 Hydrochloride Basic information |
| Product Name: | RO2959 Hydrochloride | | Synonyms: | RO2959 Hydrochloride;RO2959 HCl;IP3,SOCE,Ca2+ release-activated Ca2+ channels,RO2959 Hydrochloride,Interleukin Related,inhibit,IL-2,Stim1,RO-2959 Hydrochloride,CRAC Channel,anti-proliferation,RO 2959,Calcium release-activated channels,T-cell,RO-2959,Orai1,heart,RO2959,Inhibitor,failure;SYN5226 | | CAS: | 1219927-22-6 | | MF: | C21H20ClF2N5OS | | MW: | 463.93 | | EINECS: | | | Product Categories: | | | Mol File: | 1219927-22-6.mol |  |
| | RO2959 Hydrochloride Chemical Properties |
| storage temp. | Store at -20°C |
| | RO2959 Hydrochloride Usage And Synthesis |
| Biological Activity | RO2959 hydrochloride is a potent and selective CRAC channel inhibitor with IC50 of 402 nM. It is a potent blocker of Orai1/Stim1 channel-mediated calcium storage entry (SOCE) with IC50 of 25 nM. It is also a potent inhibitor of human IL-2 production, effectively blocking T cell receptor-triggered gene expression and T cell functional pathways. | | in vitro | RO2959 hydrochloride inhibits Orai1 and Orai3 with IC 50 values of 25 nM and 530 nM, respectively. It blocks store operated calcium entry (SOCE) in activated CD4+T lymphocytes with an IC < sub> 50 value of 265 nM.
It 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 ). | | target | | CRAC channel 402 nM (IC 50 ) | Orai1/Stim1 channels 25 nM (IC 50 ) | IL-2 | |
| | RO2959 Hydrochloride Preparation Products And Raw materials |
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