RO2959 hydrochloride structure
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Common Name | RO2959 hydrochloride | ||
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CAS Number | 1219927-22-6 | Molecular Weight | 463.931 | |
Density | N/A | Boiling Point | N/A | |
Molecular Formula | C21H19F2N5OS.xHCl | Melting Point | N/A | |
MSDS | N/A | Flash Point | N/A |
Use of RO2959 hydrochlorideRO2959 hydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM. RO2959 hydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC50 of 25 nM. RO2959 hydrochloride 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]. |
Name | 2,6-Difluoro-N-{5-[4-methyl-1-(5-methyl-1,3-thiazol-2-yl)-1,2,5,6-tetrahydro-3-pyridinyl]-2-pyrazinyl}benzamide hydrochloride (1:1) |
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Synonym | More Synonyms |
Description | RO2959 hydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM. RO2959 hydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC50 of 25 nM. RO2959 hydrochloride 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]. |
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Related Catalog | |
Target |
IC50: 402 nM (CRAC channel); 25 nM (Orai1/Stim1 channels)[1] IL-2 production[1] |
In Vitro | 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]. |
References |
Molecular Formula | C21H19F2N5OS.xHCl |
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Molecular Weight | 463.931 |
Exact Mass | 463.104523 |
Hazard Codes | Xi |
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Benzamide, 2,6-difluoro-N-[5-[1,2,5,6-tetrahydro-4-methyl-1-(5-methyl-2-thiazolyl)-3-pyridinyl]-2-pyrazinyl]-, hydrochloride (1:1) |
2,6-Difluoro-N-{5-[4-methyl-1-(5-methyl-1,3-thiazol-2-yl)-1,2,5,6-tetrahydro-3-pyridinyl]-2-pyrazinyl}benzamide hydrochloride (1:1) |